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The indole motif plays a significant role in the quest for innovative drugs. As proposed, novel N‐substituted indole derivatives were synthesized, and their efficacy against bacteria and fungi was evaluated in vitro. The synthesis of these compounds was confirmed using easily accessible building blocks, and their structural formulas were supported by corrected analytical and spectroscopic analyses. Fresh strains of Candida albicans, Escherichia coli, and Pseudomonas aeruginosa, as well as Bacillus subtilis and Staphylococcus aureus, were utilized to assess the antibacterial and antifungal activities. Notably, the derivatives 1‐(phenyl (piperidine‐1‐yl) methyl)‐1H‐indole and 4‐(1H‐indol‐1‐yl) (phenyl) morpholine have strong antifungal effects on Candida albicans that are equivalent to those of the widely used drug fluconazole. [ABSTRACT FROM AUTHOR]

Dependence on the biological activity of 2‐aminothiazole, the synthesis and chemical reactions of ethyl 3‐oxo‐3‐(thiazol‐2‐ylamino)propanoate (1) with some different reagents were described for cytotoxic and antioxidant evaluation. The new derivatives 2–19 could be synthesized and characterized by correct analytical and spectral data. In addition to the thiazole ring, these compounds contain 2H‐1,2,3‐triazole (3), 1H‐pyrazole (5, 12), 1,3‐dithiane (7), benzothiazole (10), thiazolidine (13), thiazolidinone (14, 15), 2H‐chromene (17), pyridine (19) moieties. The preparation of compounds 2–19 was performed through the formation of the isolable 2‐(2‐phenylhydrazineylidene) 2, 2‐dimethylaminomethylidene 4, 2‐phenylcarbamothioyl 9, 2‐(methylthio)(phenylamino) methylidene 11 and non‐isolable potassium bis(thiolate) 6, potassium thiolate 8 intermediates from precursor 1. The activity of these derivatives 1–19 against human lung fibroblast (WI38) and human prostate cancer (PC3) were examined in vitro using the MTT assay. The assessment of their antioxidant activities was carried out by following the ABTS method to evaluate their pharmaceutical importance. [ABSTRACT FROM AUTHOR]

Benzothiazole is the basic skeleton of multi‐target drugs with remarkable anticancer and antioxidant characteristics. In this research, new sets of benzothiazole derivatives carrying different pharmacophores and heterocyclic rings (e. g. 1,2,3‐triazole, pyrazole, thiazolidinone, thiophene, benzothiazole, 1,3‐dithiane, chromene, and pyrimidine) were efficiently synthesized through different synthetic routes from the newly synthesized ethyl 3‐(benzo[d]thiazol‐2‐ylamino)‐3‐oxopropanoate (1). These compounds were assessed in vitro as cytotoxic agents against two human cell lines, HCT‐116 (colon carcinoma) and WI‐38 (normal lung fibroblast) employing the MTT (3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide) assay, in which doxorubicin was used as a positive standard. Among the synthesized compounds, 1,2,3‐triazole 3 and pyrazoles 6 and 12 inhibited the growth of HCT‐116 cell line with high potency (IC50=7.54±0.7, 9.89±0.8, and 8.45±0.7 μM, respectively), along with low toxicity to normal cells, indicated their selectivity. Further, they were screened for their antioxidant performance using the ABTS (2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid)) bioassay and the results coincided with those of the cytotoxicity test, where the most powerful anticancer candidates displayed promising antioxidant activities with % inhibition 80.98 %, 84.12 %, and 88.82 %, respectively, comparable or superior to those of ascorbic acid (88.63 %). [ABSTRACT FROM AUTHOR]

The present review supply an overview of the chemistry of (aryl/hetaryl)thiopyran-4-one derivatives via a systematic and comprehensive survey of thesynthetic methods, the chemical reactivity and biological importance.These aryl/hetarylthiopyran-4-one derivatives that have been reported mainly from 2000 to 2019. The biological, therapeutic, and medicinal properties of (aryl/hetaryl)thiopyran-4-one derivatives and its analogues have prompted enormous research aimed at developing synthetic routes to these heterocyles. [ABSTRACT FROM AUTHOR]

In the light of using of 5‐imidazolinones in agriculture as safe and stable herbicides, the pesticide activities of some new synthesized derivatives 3‐18 of this ring system against "cotton leaf worm (Spodoptera littoralis)" have been investigated. The interpretation of the elemental and spectral analyses proved the correct structural formulae of the new synthesized compounds. The compounds 1, 5, 6a,b, 8a,c, 9, 11, 12, 15, 16, 17, and 18 showed higher potency than chlorpyrifos (dursban) recommended insecticide. While the derivatives 2, 3, 4, 7, 8b, 10, 13, and 14 showed toxicity values less than chlorpyrifos insecticide. The 5‐imidazolinones 9 and 12 may be potentially used as insecticides for treatment of cotton leaf worm. [ABSTRACT FROM AUTHOR]

The new thiopyrano[2,3-b]pyridines 4-9 could be synthesized from the nicotinonitrile derivative 1. The cytotoxicity activity of the selected compounds 5, 6 and 8 was tested against MCF-7 and HCT-116 cell lines. The compound 5 (TP5) exhibited significant inhibitory activity and displayed the most potent activity, more than 6 and 8. The compound 5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent. In the light of this result, the labeled 125I-compound 5 (125I-TP5) was prepared and its cytotoxicity against ascites tumor in mice has been evaluated. The results show that compound 5 (TP5) may be potentially used as a radiopharmaceutical for tumor diagnosis when labeled with 125I. [ABSTRACT FROM AUTHOR]

Series of novel pyrazolo[3,4‐d]pyrimidines as potential telomerase inhibitors were synthesized. Results of the antitumor assay indicated that compounds 4b, 5a–b, 13b,c, and 14a,b exhibited the most potent activity (IC50 from 39 to 43 μM) against Ehrlich ascites carcinoma cells (EAC). Also, the newly synthesized compounds were examined for telomerase inhibition by the known a TRAP assay. The results showed that compound 13c has remarkable inhibition activity with IC50 value of 30 μM. On the other hand, computational studies were performed to the titled compounds to get insight in their degree of recognition with the conserved amino acids of the telomerase enzyme active site (code: 3DU6) as promising lead in the cancer cure era. [ABSTRACT FROM AUTHOR]

An improved efficient synthesis for 2,4-azepandiones ( 3, 8, and 14) could be achieved by a careful control of the reaction conditions to cyclize ethyl 4-( N-acetylarylamino) butanoate ( 1, 7, and 13), respectively. The ethyl 4-arylamino butanoate ( 9 or 12) was prepared by stirring the ethyl 4-bromobutanoate and substituted anilines at room temperature. Then, they were acetylated with and triethylamine under the conditions that avoid the formation of 2-pyrrolidinone derivatives 10. Due to the rapid decomposition of the acetylated product ( 7 or 13) to its starting material ( 9 or 12), the reaction mixture is directly transferred without workup to the next step. The azepandione synthesis is favored by using a weak base at low temperature, where it is in a competition with the other modes of ring closure. The structures of the new compounds were supported by correct analytical and spectral data. [ABSTRACT FROM AUTHOR]

The focus of this review is on the structure, methods of syntheses, chemical reactivity, and biological activity of 2,4-azepandione and some derivatives. Some important fused-ring systems containing 2,4-azepandione moiety were also reviewed. [ABSTRACT FROM PUBLISHER]

An allopurinol locked nucleic acid (LNA) monomer was prepared by a novel strategy through C6 deamination of the corresponding 8-aza-7-bromo-7-deazaadenine LNA monomer with aqueous sodium hydroxide. An 8-aza-7-deazaadenine LNA monomer was also synthesized by a modification of the new synthetic pathway. N-Glycosylation at the 8-position was prevented by steric hindrance from the 7-bromo atom in the starting material 8-aza-7- bromo-7-deazaadenine. In the final step of the synthesis, the bromine was removed together with a benzyl protecting group by catalytic reduction with ammonium formate to give the required LNA monomers. [ABSTRACT FROM AUTHOR]

A new protocol was developed for the synthesis of azo pyrazole derivatives via one-pot reaction of β-ketonitriles and phenyl hydrazines in the presence of nano SiO 2 as a mild catalyst. The synthesized dyes were elucidated using spectrophotometry, mainly NMR; FTIR; UV as well as elemental analysis. The dyeing was carried out utilizing supercritical carbon dioxide as a green medium. Outstanding deep color shades and excellent dye fixation were exhibited by all new dyes. Furthermore, the dyed samples revealed superlative color fastness. The biological evaluation of both the dyestuffs and the dyed samples showed overgrowing antimicrobial activity against the tested microorganisms. Therefore, our findings assured that disperse reactive dyes are the most commercially appropriate materials for dyeing cotton in supercritical carbon dioxide. [Display omitted] • Azo pyrazole catalyzed with (SiO 2 - NPs) was used for dyeing cotton in scCO 2. • Both the dyestuffs and the dyed samples showed excellent antimicrobial activities. • Raman spectroscopy excluded ring dyeing. [ABSTRACT FROM AUTHOR]

• Changes of absorbances and melting points were not related to color differences. • Changes in solubilities and affinities were fundamental reason for color differences. • Degree of esterification had greatest effect on disperse red 167:1′s color difference. [Display omitted] The reason of color differences caused by different degree of esterification disperse dyes were investigated by disperse orange 30, disperse red 167:1, disperse blue 79:1 with different degree of esterification. The results showed that the changes of light absorbance abilities and melting points caused by ester groups had no obvious correlation with the color differences caused by ester groups. The changes in the solubilities and affinities caused by the ester groups were the fundamental reason for the changes in the dyeing properties of disperse orange 30, disperse red 167:1 and disperse blue 79:1. As a joint result of the decrease in solubilities and affinities, the dye sorption in polyethylene terephthalate of unesterified disperse orange 30, unesterified disperse red 167:1 and unesterified disperse blue 79:1 were reduced by 37.7%, 83.6% and 54.6%, respectively, compared with those of the corresponding completely esterified dyes. [ABSTRACT FROM AUTHOR]

Background: Nucleophosmin1 (NPM1) protein encoded from the NPM1 gene is a ubiquitously expressed nucleolar phoshoprotein which shuttles continuously between the nucleus and cytoplasm. NPM1 protein plays an important role in cell proliferation and apoptosis. NPM1 gene mutations at exon 12 represent the hallmark of a large sub-group of cytogenetically normal acute myeloid leukemia (CN-AML) patients worldwide., Methods: Genomic DNA from 53 CN-AML patients were amplified by PCR and followed by fragment analysis of post-PCR products using GeneMapper software for detection of NPM1 mutations., Results: NPM1 exon 12 mutations were found are 15/53 CN-AML patients (28.3%) including 3 of M1, 3 of M2, 5 of M4, 3 of M5, and 1 of M6 FAB subtypes. The NPM1 mutation was significantly associated with lower relapse rate (p < 0.05). The complete remission (CR) rate was significantly higher in the patients with high NPM1 mutation load (> 50%) than low NPM1 mutation load (< 50%) (87.5% vs. 28.6%; p = 0.02)., Conclusions: The aim of this study was to evaluate the NPM1 gene exon 12 mutation in Egyptian patients with CN-AML and its relation to clinical characteristics and patient outcome and survival.

Background: Recently various molecular markers and global gene expression profiling have been investigated to improve risk profile characterization of AML with normal cytogenetics. Our main objective is to investigate the prognostic impact of brain and acute leukemia, cytoplasmic (BAALC) expression in AML with normal karyotype., Methods: BAALC expression was analysed using quantitative real time (QRT) PCR., Results: High expression was detected in 22 of 45 patients (48.9%) and its expression did not correlate with the clinical parameters of patients. High BAALC expressers had significantly lower incidence of CR (22.7% vs. 73.9%; p = 0.001), higher mortality rate (72.1% vs. 39.1%; p = 0.023), showed significantly shorter DFS (mean 4.5 vs. 13.21 months, p < 0.001), and inferior overall survival (7.02 vs. 15.02 months, p < 0.001). Multivariable analysis confirmed high BAALC expression as an independent risk factor for DFS and OS., Conclusions: BAALC expression is an important prognostic factor in AML patients with normal karyotype and its incorporation into novel risk-adapted therapeutic strategies will improve the currently disappointing cure rate of this group of patients.