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The present study is an effort to explore some low molecular weight chemical entities quinazolinone incorporated naphthyl chalcones for their cytotoxic potential and, that can act smartly by inhibiting the mutated molecular targets EGFR (T790M mutation; PDB Id: 5Y9T), and mutated K-RAS(G12D mutation; PDB Id: 4EPT). The in-vitro cytotoxic studies were done by the MTT assay method. For the lung cancer cell lines (A549), N1-N4 were found as more potent than the reference erlotinib (IC50:44.4μg/ml), and among them, the most potent compound is N3 (IC50:11.29 μg/ml). Against the colorectal cancer cell lines (Caco2), the same compound N3 was found as most potent (IC50:10.79 μg/ml). Molecular docking by autodock-4 revealed that all the title compounds have high affinity for both the molecular targets, as they have high negative binding energies. The inhibition constants obtained in docking studies are in nanomoles, The title compounds can be used as a template for developing more potent, selective and dual targeted drugs to treat lung cancer and colorectal cancer.

Funding: SERB-DST (Science and Engineering Research Board-Department of Science and Technology), Govt. of India, is duly acknowledged for financial assistance under Fast Track Scheme For Young Scientist (to Dr. Prabodh Chander Sharma) video file No.: SB/FT/CS-134/2012 dated: July 15, 2014. Cancer is one of the life-threatening diseases accountable for millions of demises globally. The inadequate effectiveness of the existing chemotherapy and its harmful effects has resulted in the necessity of developing innovative anticancer agents. Thiazolidin-4-one scaffold is among the most important chemical skeletons that illustrate anticancer activity. Thiazolidin-4-one derivatives have been the subject of extensive research and current scientific literature reveals that these compounds have shown significant anticancer activities. This manuscript is an earnest attempt to review novel thiazolidin-4-one derivatives demonstrating considerable potential as anticancer agents along with a brief discussion of medicinal chemistry-related aspects of these compounds and structural activity relationship studies in order to develop possible multi-target enzyme inhibitors. Most recently, various synthetic strategies have been developed by researchers to get various thiazolidin-4-one derivatives. In this review, the authors highlight the various synthetic, green, and nanomaterial-based synthesis routes of thiazolidin-4-ones as well as their role in anticancer activity by inhibition of various enzymes and cell lines. The detailed description of the existing modern standards in the field presented in this article may be interesting and beneficial to the scientists for further exploration of these heterocyclic compounds as possible anticancer agents. Publisher PDF

A new series of (E)-6-methyl-N-((3-phenyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol-4-yl)methylene)benzo[d]thiazol-2-amine derivatives was developed. Structural investigation of the synthesized derivatives was carried out by several instrumental method of analysis like IR, and 1H-NMR spectroscopy. The titled analogues were examined for in-vitro anticancer and antiinfective activities. The biological findings specified that analogues 5a, 5b, 5d, 5e, 5f and 5g showed most potent antibacterial activity (MIC 62.5-250μg/mL) and 5a, 5e, 5f and 5g displayed most potent antifungal action (MIC 62.5-500 μg/mL) than standard drugs. Compounds 5a and 5e were reported to be most active antimalarial analogue having IC50 value of 0.24-0.49μg/mL. Compounds 5a, 5e and 5f showed shortest mean paralysis time of (25.6±4.56 min, 26.4±4.97 min and 26.8±4.76 min) and mean death time (47.6±8.01min, 45.6±3.04min and 46.6±7.40min), respectively. Compound 5e showed moderate cytotoxicity with IC50 value of 65.4 against MCF-7. The results proved that 1,3-thiazolyl-pyrazole clubbed benzothiazole derivatives showed considerable antiinfective and cytotoxic activity. Keywords: Anti-infective activity, Cytotoxic activity, Spectroscopic methods, Thiazole, Pyrazole, Benzothiazole.

The quinoline scaffolds are privileged for their numerous biological activities in the pharmaceutical field. This moiety constitutes a well-known space in several marketed preparations. The quinoline scaffolds gained attention in modern days being an important chemical moiety in the identification, designing, and synthesis of novel potent derivatives. The current review is developed to shine the light on critical and significant insights on the quinoline derivatives possessing diverse biological activities such as analgesic, anti-inflammatory, antialzheimer, anti-convulsant, anti-oxidant, antimicrobial, anti-cancer activities and so on. A detailed summary of quinoline ring from its origin to the recent advancements regarding its synthesis, green chemistry approaches, patented methods, and its marketed drugs is presented in the review. We attempted to review the literature compiling the critical information that has potential to encourage fellow researchers and scientists for the design and development of quinoline scaffold based active molecules that have improved therapeutic performance along with profound pharmacological properties.

HDAC inhibitors (HDACi) play an essential role in various cellular processes, such as differentiation and transcriptional regulation of key genes and cytostatic factors, cell cycle arrest and apoptosis that facilitates the targeting of epigenome of eukaryotic cells. In the majority of cancers, only a handful of patients receive optimal benefit from chemotherapeutics. Additionally, there is emerging interest in the use of HDACi to modulate the effects of ionizing radiations. The use of HDACi with radiotherapy, with the goal of reaching dissimilar, often distinct pathways or multiple biological targets, with the expectation of synergistic effects, reduced toxicity and diminished intrinsic and acquired resistance, conveys an approach of increasing interest. In this review, the clinical potential of HDACi in combination with radiotherapy is described as an efficient synergy for cancer treatment will be overviewed.

Background The World Health Organization (WHO) announced the COVID-19 occurrence as a global pandemic in March 2020. The treatment of SARS-CoV-2 patients is based on the experience gained from SARS-CoV and MERS-CoV infection during 2003. There is no clinically accepted therapeutic drug(s) accessible yet for the treatment of COVID-19. Main body Corticosteroids, i.e., dexamethasone, methylprednisolone, hydrocortisone and prednisone are used alone or in combination for the treatment of moderate, severe and critically infected COVID-19 patients who are hospitalized and require supplemental oxygen as per current management strategies and guidelines for COVID-19 published by the National Institutes of Health. Corticosteroids are recorded in the WHO model list of essential medicines and are easily accessible worldwide at a cheaper cost in multiple formulations and various dosage forms. Corticosteroid can be used in all age group of patients, i.e., children, adult, elderly and during pregnancy or breastfeeding women. Corticosteroids have potent anti-inflammatory and immunosuppressive effects in both primary and secondary immune cells, thereby reducing the generation of proinflammatory cytokines and chemokines and lowering the activation of T cells, monocytes and macrophages. The corticosteroids should not be used in the treatment of non-severe COVID-19 patients because corticosteroids suppress the immune response and reduce the symptoms and associated side effects such as slow recovery, bacterial infections, hypokalemia, mucormycosis and finally increase the chances of death. Conclusion Intensive research on corticosteroid therapy in COVID-19 treatment is urgently needed to elucidate their mechanisms and importance in contributing toward successful prevention and treatment approaches. Hence, this review emphasizes on recent advancement on corticosteroid therapy for defining their importance in overcoming SARS-CoV-2 pandemic, their mechanism, efficacy and extent of corticosteroids in the treatment of COVID-19 patients.

Background:Objective: Various natural gums can be synergistically used in nanoparticulate drug delivery systems to treat cardiovascular diseases. Nanotechnology has been integrated into healthcare in terms of theranostics. In this review, we consider various natural gums that can be used for the preparation of nanoparticles and their role to treat cardiovascular disease.Methods:Nanoparticles can carry drugs at nanoscales and deliver them to the targeted sites with the desired pattern of drug release. They have specialized uptake mechanisms (e.g. - absorptive endocytosis) which improve the bioavailability of drugs.Results:By considering cardiovascular diseases at the molecular level, it is possible to modify the materials with nanotechnology and apply nano-formulations efficiently as compared with conventional preparations, due to the fact that the extracellular matrix (ECM) comprises components at the nanoscale range. The interactions of ECM components with cellular components occur at the nanoscale, therefore the nanomaterials have the potential to maintain the nanoscale properties of cells. The synthetic materials used to develop the nanoparticulate drug delivery system may cause toxicity.Conclusion:This problem can be overcome by using natural polymers. Natural gums can be used in nanoparticulate drug delivery systems as reducing and stabilizing agents and in some cases; they may directly or indirectly influence the rate of drug release and absorption from the preparation.

Background: Thiazole is widely investigated bioactive scaffold and dynamic tool in medicinal chemistry research. Significance of thiazole compounds are well documented as thiazole is an obligatory structure of number of currently available therapeutics. In spite of that, thiazole derivatives are endowed with myriad biological activities, such as antiviral, anticancer, antibacterial, antifungal, antimalarial, antiparkinsonian, anti-inflammatory activities and many more. Methods: In recent past, different approaches have been introduced for synthesis of thiazole and related compounds. Intrinsic molecular interaction between newly synthesized thiazole compounds and plethora of drug targets/enzymes has rendered discovery of new drug molecules with advances in modes of action. A renewed interest in therapeutic use of thiazole derivatives has been seen among the prospective researchers as exemplified by influx of huge scientific articles and patents. Some important patents of anti-infective and anticancer interest have been addressed appropriately and are presented in tables. Results: This review paper is a contemporary approach on therapeutic/applications of thiazole derivatives by summarizing important patents filed from 2000-2017. The main focus of these patents is on anti-infective and anticancer potential of thiazole based compounds. Conclusion: These approaches may provide valuable information for the further design of more active biological agents through various modifications and derivatizations.

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)-caused Coronavirus Disease 2019 (COVID-19) is currently a global pandemic that has wreaked havoc on public health, lives, and the global economy. The present COVID-19 outbreak has put pressure on the scientific community to develop medications and vaccinations to combat COVID-19. However, according to highly optimistic forecasts, we could not have a COVID-19 vaccine until September 2020. This is due to the fact that a successful COVID-19 vaccine will necessitate a careful validation of effectiveness and adverse reactivity given that the target vaccine population includes high-risk people over 60, particularly those with severe co-morbid conditions, frontline healthcare professionals, and those involved in essential industrial sectors. For passive immunization, which is being considered for Covid-19, there are several platforms for vaccine development, each with its own advantages and disadvantages. The COVID-19 pandemic, which is arguably the deadliest in the last 100 years after the Spanish flu, necessitates a swift assessment of the various approaches for their ability to incite protective immunity and safety to prevent unintended immune potentiation, which is crucial to the pathogenesis of this virus. Considering the pandemic's high fatality rate and rapid spread, an efficient vaccination is critical for its management. As a result, academia, industry, and government are collaborating in unprecedented ways to create and test a wide range of vaccinations. In this review, we summarize the Covid-19 vaccine development initiatives, recent trends, difficulties, comparison between traditional vaccines development and Covid-19 vaccines development also listed the approved/authorized, phase-3 and pre-clinical trials Covid-19 vaccines in different countries.

It is a major concern to treat cancer successfully, due to the distinctive pathophysiology of cancer cells and the gradual manifestation of resistance. Specific action, adverse effects and development of resistance has prompted the urgent requirement of exploring alternative anti-tumour treatment therapies. The naturally derived microbial toxins as a therapy against cancer cells are a promisingly new dimension. Various important microbial toxins such as Diphtheria toxin, Vibrio cholera toxin, Aflatoxin, Patulin, Cryptophycin-55, Chlorella are derived from several bacterial, fungal and algal species. These agents act on different biotargets such as inhibition of protein synthesis, reduction in cell growth, regulation of cell cycle and many cellular processes. Bacterial toxins produce actions primarily by targeting protein moieties and some immunomodulation and few acts through DNA. Fungal toxins appear to have more DNA damaging activity and affect the cell cycle. Algal toxins produce alteration in mitochondrial phosphorylation. In conclusion, microbial toxins and their metabolites appear to have a great potential to provide a promising option for the treatment and management to combat cancer.

Fluoroquinolones are of pivotal interest for scientists because of their excellent pharmacological and pharmacokinetic profiles. They have a broad spectrum of antimicrobial activity and show several promising features such as, greater bioavailability, admirable tissue penetration and comparatively lower incidence of antagonistic and lethal effects. These have made the compounds highly desirable to combat several infectious diseases. Various synthetic conventions have been established to hasten the fluoroquinolone’s amination rate and to improve yield. Such methods have significant disadvantages including, costly reagents, usage of vast quantities of harmful solvents, excessive heat and sideways reactions. These drawbacks aren’t appropriate in current pharmaceutical market. Hence, it is highly desirable to develop a newer green and more efficient process for fluoroquinolones synthesis. Green chemistry methodology endeavours to achieve sustainability at the molecular level. The field of green chemistry has shown how chemists can design next-generation products and processes to make them more cost-effective while being virtuous for human health and the environment. This graphical review demonstrates the current developments in the synthesis of fluoroquinolones employing the principles of green chemistry by using the novel, recyclable and environmental-friendly catalysts and solvents.

The novel coronavirus disease-19 (COVID-19) is a global pandemic that emerged from Wuhan, China, and has spread all around the world, affecting 216 countries or territories with 21,732,472 people infected and 770,866 deaths globally (as per WHO COVID-19 updates of August 18, 2020). Continuous efforts are being made to repurpose the existing drugs and develop vaccines for combating this infection. Despite, to date, no certified antiviral treatment or vaccine exists. Although, few candidates have displayed their efficacy in in vitro studies and are being repurposed for COVID- 19 treatment. This article summarizes synthetic and semi-synthetic compounds displaying potent activity in clinical uses or studies on COVID-19 and also focuses on the mode of action of drugs being repositioned against COVID-19.

Background Fluoroquinolones, the synthetic antibacterial agents are being successfully utilized against bacterial infections, since the time immemorial. Despite of enormous useful features, these drugs are associated with some limitations also. Large number of efforts has been made by various scientists to improve pharmacokinetic properties of these drugs and hence, to overcome the limitations associated with them. Objectives The aim of this paper is to introduce a novel scheme for synthesis of prodrug with improved pharmacokinetic properties i.e., lipophilicity and consequently, modified bioavailability of norfloxacin. Methods Fatty acid hydrazide of selected fatty acid was synthesized followed by preparation of 5-formyl salicylamide. N-Mannich base of norfloxacin was synthesized by reacting norfloxacin with 5-formyl salicylamide. The prodrug was obtained by covalently coupling this N-Mannich base of norfloxacin with fatty acid hydrazide. The synthesized lipid based prodrug was evaluated for partition coefficient by shake flask method and screened for antimicrobial activity against selected strains. Drug content determination and in vitro dissolution studies utilizing HPLC were also carried out. Results The synthesized prodrug was found to exhibit improved partition coefficient (1.15) when compared with parent drug, norfloxacin (0.46). The results of antimicrobial evaluation indicate promising antibacterial and antifungal activity. Conclusion The synthesized prodrug proved to be a good antimicrobial substance due to improved lipophilicity and would be expected to be used as a suitable candidate for exploration of possible utilities in treatment of bacterial infections in forthcoming time.

The exhaustive exploration of the conventional synthetic approaches for the synthesis of nitrogen and sulphur containing heterocyclic moieties has diverted the attention of researchers towards novel eco-friendly strategies of these compounds. Several green chemistry-based synthetic methods like multi-component single pot reaction, recyclable green-based catalyst, green solvent, reusable solvent, ultrasound-mediated synthesis, the solvent-free and microwave-assisted technique have been developed for the synthesis of thiazole derivatives with anticancer potential. According to the cancer society, almost 14.1 million cancer cases and about 8.2 million deaths due to cancer have been reported, which implies that one of every seven deaths occurs due to cancer disease. The thiazole scaffold is contained in more than 18 FDA-approved drugs, as well as, in several experimental formulations. Among them, alpelisib, a thiazole-based drug with the brand name Pigray®, was approved in 2019 for the treatment of breast cancer. The goal of the present review is to highlight the recent advancements in the green chemistry-based synthesis of thiazole derivatives with the discussion of their structure-activity relationship. Based on innovative eco-friendly reports in synthetic literature, this paper compiled the green strategies-based development of thiazole derivatives from 2012 till now with effective anticancer potential.

The structure and ligand based synergistic approach is being applied to design ligands more correctly. The present report discloses the combination of structure and ligand based tactics i.e., molecular docking, energetic based pharmacophore, pharmacophore and atom based 3D-QSAR modeling for the analysis of thiophene derivatives as anticancer agent. The main purpose of using structure and ligand based synergistic approach is to ascertain a correlation between structure and its biological activity. Thiophene derivatives have been found to possess cytotoxic activity in several cancer cell lines and its mechanism of action basically involves the binding to the colchicine site on β-tubulin. The structure based approach (molecular docking) was performed on a series of thiophene derivatives. All the structures were docked to colchicine binding site of β tubulin for examining the binding affinity of compounds for antitumor activity. The pharmacophore and atom based 3D-QSAR modeling was accomplished on a series of thiophene (32 compounds) analogues. Five-point common pharmacophore hypotheses (AAAAR.38) were selected for alignment of all compounds. The atom based 3D-QSAR models were developed by selection of 23 compounds as training set and 9 compounds as test set, demonstrated good partial least squares statistical results. The generated common pharmacophore hypothesis and 3D-QSAR models were validated further externally by measuring the activity of database compounds and assessing it with actual activity. The common pharmacophore hypothesis AAAAR.38 resulted in a 3D-QSAR model with excellent PLSs data for factor two characterized by the best predication coefficient Q2 (cross validated r2) (0.7213), regression R2 (0.8311), SD (0.3672), F (49.2), P (1.89E-08), RMSE (0.3864), Stability (0.8702), Pearson-r (0.8722). The results of these molecular modeling studies i.e., molecular docking, energetic based pharmacophore, pharmacophore and atom based 3D-QSAR modeling would be fruitful to improve the pharmacophore for design of novel combretastatin A-4 based thiophenes for anticancer activity.

Docking studies are proved to be an essential tool that facilitates the structural diversity of natural products to be harnessed in an organized manner. In this study, pyridoacridines containing natural anticancer pigments were subjected to docking studies using Glide (Schrodinger). Investigations were carried out to find out the potential molecular targets for these selected pigments. The docking was carried out on different cancer macromolecules involved in different cell cycle pathways, that is, CDK-2, CDK-6, Bcl-2, VEGFR-2, IGF-1R kinase, and G-Quadruplexes. CDK-6 was found to be the most suitable anticancer target for the pyridoacridines. In addition, effectiveness of the study was further evaluated by performing docking of known inhibitors against their respective selected macromolecules. However, the results are preliminary and experimental evaluation will be carried out in near future.

Background: Severity of microbial infections and escalating resistance towards antibiotics has created a deep necessity for discovery of novel anti-infective agents. Heterocyclic chemistry of benzothiazole has become one of the most prolific areas in the field of drug discovery and development that has attracted great attention in recent time due to its increasing importance in the field of pharmaceuticals. Method: The importance of benzothiazole and derivatives as potential antimicrobial agents has been well established and a large number of papers have been published in this regard. Result: The present communication is an earnest attempt to review the chemistry, synthetic aspects including click chemistry and antimicrobial activities of benzothiazole derivatives reported in recent scientific literature. Conclusion: The scientific information of this manuscript may be worthwhile in encouraging the prospective researchers working on this heterocyclic scaffold.

Quinolones and fluoroquinolones are principal weapons against variety of bacterial infections and exert their antibacterial potential by interfering the activities of bacterial enzymes. As these agents are associated with some limitations, an important approach to overcome these major constraints is to prepare covalent derivatives, i.e. prodrugs. Prodrug design has been employed to improve the limitations of these drugs such as less aqueous solubility, poor absorption and distribution, toxicity, disagreeable taste, poor lipophilicity etc and for improving their pharmacological profile. This paper highlights the utility of various prodrug strategies in optimizing the therapeutic index of these antibacterial agents and their recent patents. Some of their prodrugs being utilized at preclinical and clinical levels have also been discussed. Hence, this paper has been prepared to present the significant findings of various research papers that would be helpful in motivating scientific researchers to forward the research in direction of utilization of prodrugs in clinical therapy.

Despite the adverse effects of microbial hazards on public health, major pharmaceutical firms have left the field of anti-infective development and a dramatic reduction in the number of researcher's intricated in the quest for new specific anti-infective leads. In the non-existence of an efficient forum for antibiotics development and over usage in human beings and animals, bacteria have demoralized this potential by gradually establishing the resistance toward most of the antibiotics used. Thus, the production of novel and successful anti-infective drugs is urgently required to combat this resistance. Hydrazones and hydrazides have mounted as a key-skeleton for the development of active drugs, due to their important biological and pharmacological profiles. Hydrazones are being manufactured as medicines by various investigators to fight against the ailments with maximal effects and minimal toxicity. This paper focuses on the outline of the literature results of recent years, incorporating the work on the anti-infective profile of hydrazone analogues. This review may also act as an excellent basis for the development of new derivatives of hydrazone as potential anti-infective mediators.

In the pasture of oncology, anticancer agents having advanced modes of action are of great interest because of increasing chronicity of resistance against anticancer drugs. Heterocyclic scaffolds like benzothiazoles are reported to display an extensive range of pharmacological activities including anticancer, anti-tubercular, antiviral, fungicidal, etc. and are indispensable tools for the researchers involved in vistas of chemistry for proposing of novel anticancer drugs. Benzothiazole scaffold is a bicyclic organic compound having benzene ring fused with heterocyclic nucleus (thiazole) containing sulphur and nitrogen atoms that possess a wide range of different pharmacological activities and are still of grand and logical concern nowadays. Interesting pharmacological activities are exhibited by benzothiazoles and they were developed as successful inhibitors of a variety of biological targets such as tubulin polymerase inhibitor, DNA topoisomerase-inhibitor, an Abl kinase inhibitor, HDAC inhibitor, Aurora-B kinase inhibitor. This review highlights the latest research on the structure-activity relationship of benzothiazole scaffold against different biological targets for their anticancer activity. This survey additionally addresses the recent patents granted and novel advancement made through the application of nanocarriers in recent decades with thorough talk of benzothiazoles as conceivable anticancer mediators which may be helpful for the emerging scientific pursuits.

Cancer is a very risky life-threatening disease having most formidable afflictions in the world. Several anticancer agents are commercially accessible, however, the emergence of acquired drug resistance along with extreme adverse effects of these clinically used anticancer medications are major barriers to the effective chemotherapy. Thus, it is recommended to rationally design the newer drugs with few side effects. Fluoroquinolone derivatives are of pivotal interest for researchers due to their admirable pharmacological and pharmacokinetic profiles. They exhibit several favourable characteristics including, higher bioavailability, excellent tissue penetration and relatively low prevalence of adverse and toxic effects. Due to their potential interventions in carcinogenesis and mutagenesis, the focus of the area of research is nowadays shifting towards anticancer aspects of these compounds. This review shows the recent advancements in the development of novel fluoroquinolones as potential anticancer and cytotoxic agents and structure-activity relationships along with the possible modes of action for further development and recent patents filed/granted related to anticancer activity from the last few years have also been tabulated. Also, this review is an attempt to focus on the various upcoming aspects of fluoroquinolones and provides a newer outlook on the possible roles of fluoroquinolones in the treatment of cancer. Scientific information identified in this paper is expected to be useful for aspiring researchers working on the anticancer activity of fluoroquinolones.

Fourteen N-[{(substituted-phenylthiazol-2-yl)-3-aryl-1H-pyrazol-4-yl}methylene]-5-substituted-thiazol-2-amine (5a-n) analogs were synthesized by the reaction of 3-aryl-1-(thiazol-2-yl)-1H-pyrazole-4-carbaldehyde and substituted thiazole amines. The structures of prepared compounds were delineated by elemental analysis, FT-IR and 1H NMR spectra. These analogs were scrutinized for in vitro anti-infective and cytotoxic activities. Some thaizole clubbed pyrazole derivatives were assessed for their cytological changes in germ cells of Capra hircus by using histomorphological analysis, fluorescence assay and apoptosis quantification. Compound 5l having 4-NO2 substituent induced the significant apoptosis in tested cells of Capra hircus. The results revealed that compounds 5c, 5e, 5k, and 5l have commendable antibacterial activity within MIC range of 62.5–250 μg/ml. Compound 5c emerged as a potent antimalarial compound by exhibiting IC50 value of 0.23 μg/ml and compound 5j induced paralysis of Pherentima posthuma at 8.6 ± 1.94 min and death at 20 ± 5.04 min, respectively. Compound 5j revealed an excellent cytotoxicity at IC50 value of 30.7 and

In the last few decades, considerable progress has been made in anticancer agents development, and several new anticancer agents of natural and synthetic origin have been produced. Among heterocyclic compounds, thiazole, a 5-membered unique heterocyclic motif containing sulphur and nitrogen atoms, serves as an essential core scaffold in several medicinally important compounds. Thiazole nucleus is a fundamental part of some clinically applied anticancer drugs, such as dasatinib, dabrafenib, ixabepilone, patellamide A, and epothilone. Recently, thiazole-containing compounds have been successfully developed as possible inhibitors of several biological targets, including enzyme-linked receptor(s) located on the cell membrane, (i.e., polymerase inhibitors) and the cell cycle (i.e., microtubular inhibitors). Moreover, these compounds have been proven to exhibit high effectiveness, potent anticancer activity, and less toxicity. This review presents current research on thiazoles and elucidates their biological importance in anticancer drug discovery. The findings may aid researchers in the rational design of more potent and bio-target specific anticancer drug molecules.