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Phytochemical investigation of the stem bark of Anthocephalus cadamba(Rubiaceae) led to the isolation of total ten secondary metabolites (1‐10) including β–sitosterol (1), ursolic acid (2), vanillic acid (3), quinovic acid (4), 3‐O‐[α‐L‐rhamnopyranosyl]‐quinovic acid (5), β‐sitosterol β‐D‐glucoside (6), cadambine (7), 3β‐dihydrocadambine (8), 7‐O‐acetyl loganin (9) and hexyl p‐coumarate (10). Four acetylated derivatives 2 a,5 a,7 aand8 aobtained through acetylation of compounds 2, 5, 7 and 8 respectively. All the compounds characterized using 1H and 13CNMR, HRESIMS and IR and comparison with literature. Compound 4showed the best cytotoxic activity with IC50 value 4 and 7 μM against pancreatic (MIA‐pa‐Ca‐2) and leukemia (HL‐60) cancer cells respectively. Docking results supported the anticancer potential of compound 4via inhibition of EGFR receptor (PDB ID:3POZ) and its pharmacokinetic profile found optimized as per the Lipinski's filter. Therefore compound 4has the potential to be developed as an anticancer agent against pancreatic cancer cells. [ABSTRACT FROM AUTHOR]

Phytochemical investigation of Psoralea corylifolia seeds as a potential source of anticancer lead molecules led to the isolation of total fourteen secondary metabolites (1–14) bakuchiol (1), isopsoralen (2), psoralen (3), bavachinin (4), 4‐O‐methylbavachalcone (5), bavachalcone (6), 12, 13‐Dihydro‐12, 13‐epoxybakuchiol (7), corylin (8), psoralidin (9) neocorylin (10), corylifol A (11), neobavaisoflavone (12), bavachin (13) and 12‐hydroxyisobakuchiol (14). Their structures were confirmed by 1DNMR, MASS spectra and comparison with the literature. Compounds 10, 11, 13 and 14 exhibited promising in vitro anticancer activity further supported by in‐silico docking results against BRCA‐1 (PDB ID: 4OFB). Bavachin 13 was found as the most promising cytotoxic metabolite with IC50 value 2.22 μM against MCF‐7 cells. In‐vitro mechanism of action studies of 13 against MCF‐7 cell line showed apoptotic cleavage. In addition, most of the compounds showed good ADMET and drug likeness profile. Cumulative in‐vitro and in‐silico results provided compound 13 as a potential anticancer agent against breast cancer cells. [ABSTRACT FROM AUTHOR]

Due to its appreciable diversity in biological actions, thiazole and its substituted components, a significant class of heterocyclic compounds has developed as an influential scaffold in the field of chemical sciences. The variability of thiazole core has been expressed through the effective instigation of its anticancer (Dasatinib, Tiazofurin), antiretroviral (Ritonavir, Brecanavir), antimicrobial (Sulfathiazole, Ravuconazole) and anti‐inflammatory (Fenclozic acid, Meloxicam) derivatives. This reasonable diversity in the physiological reaction pattern led many scientists to refine and develop new structural alternatives with much more efficient pharmacological action. This review is crucial for previous studies and projects to survey the antimicrobial activity of thiazole and thiazole related compounds to the mid of 2019. [ABSTRACT FROM AUTHOR]