Synthesis, cytotoxicity and antimicrobial evaluation of new coumarin-tagged β-lactam triazole hybrid.

Synthesis, cytotoxicity and antimicrobial evaluation of new coumarin-tagged β-lactam triazole hybrid. Chem Biodivers. 2019 Dec 01;: Authors: Dhawan S, Awolade P, Kisten P, Cele N, Pillay AS, Saha ST, Kaur M, Jonnalagaddas SB, Singh P Abstract A series of coumarin-tagged β-lactam triazole hybrids ( 10a - o ) were synthesized and tested for their cytotoxic activity against MDA-MB-231 (triple negative breast cancer), MCF-7 (estrogen receptor positive breast cancer (ER+) and A549 cells (human lung carcinoma) cancer cell lines including a normal cell line, HEK-293 (human embryonic kidney). Two compounds, 10b and 10d exhibited substantial cytotoxic effect against MCF-7 cancer cell-line with IC 50 values of 53.55 and 58.62 µM, respectively. More importantly, compounds 10b and 10d were non-cytotoxic against HEK-293 cells. Structure-activity relationship (SAR) studies suggested that the nitro and chloro group at the C-3 position of phenyl ring are favorable for anticancer activity, particularly against MCF-7 cell-line. Furthermore, antimicrobial evaluation of these compounds revealed modest inhibiton of examined pathogenic strains with compounds 10c and 10i being the most promising antimicrobial agents against Pseudomonas aeruginosa and Candida albicans respectively. PMID: 31788939 [PubMed - as supplied by publisher]
Source: Chemistry and Biodiversity - Category: Biochemistry Authors: Tags: Chem Biodivers Source Type: research