Green, facile synthesis and evaluation of unsymmetrical carbamide derivatives as antimicrobial and anticancer agents with mechanistic insights
Farid M. Sroor,
Ahmed A. F. Soliman,
Elham Mohamed Youssef
et al.
Abstract:A very practical method for the synthesis of unsymmetrical carbamide derivatives in good to excellent yield was presented, without the need for any catalyst and at room temperature. Using a facile and robust protocol, fifteen unsymmetrical carbamide derivatives (9–23) bearing different aliphatic amine moieties were designed and synthesized by the reaction of secondary aliphatic amines with isocyanate derivatives in the presence of acetonitrile as an appropriate solvent in good to excellent yields. Trusted inst… Show more
Four pyrazol derivatives (4, 5, 7, and 25) showed potent anti-PACA-2 cell line with IC50 (13.0, 31.5 and 24.9, 5.5 μg mL−1) respectively, while compounds 23 and 25 showed potent anti-PC3 cell line with IC50 (26.1 and 11.8 μg mL−1).
Four pyrazol derivatives (4, 5, 7, and 25) showed potent anti-PACA-2 cell line with IC50 (13.0, 31.5 and 24.9, 5.5 μg mL−1) respectively, while compounds 23 and 25 showed potent anti-PC3 cell line with IC50 (26.1 and 11.8 μg mL−1).
A new series of pyrazole-based chalcones were synthesized and tested against MCF7, PC3, PACA2 and BJ1 as in vitro study. Gene expression, DNA damage, DNA fragmentation and molecular docking for were discussed.
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