Chemistry and biodiversity (2020)
Update date:2022-09-26
Topics: Synthesis Triazole Cytotoxicity Antimicrobial Evaluation Coumarin β-Lactam
Awolade, Paul
Cele, Nosipho
Dhawan, Sanjeev
Jonnalagadda, Sreekantha B.
Kaur, Mandeep
Kisten, Prishani
Pillay, Ashona-Singh
Saha, SouravTaru
Singh, Parvesh
A series of coumarin-tagged β-lactam triazole hybrids (10a–10o) 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 (human lung carcinoma) cancer cell lines including one normal cell line, HEK-293 (human embryonic kidney). Two compounds 10b and 10d exhibited substantial cytotoxic effect against MCF-7 cancer cell lines with IC50 values of 53.55 and 58.62 μm, respectively. More importantly, compounds 10b and 10d were non-cytotoxic against HEK-293 cell lines. 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 lines. Furthermore, antimicrobial evaluation of these compounds revealed modest inhibition of examined pathogenic strains with compounds 10c and 10i being the most promising antimicrobial agents against Pseudomonas aeruginosa and Candida albicans, respectively.
View MoreWuhan Fortuna Chemical Co.,Ltd
website:http://www.fortunachem.com
Contact:86-27-59207850
Address:Add: Room 2015, No.2 Building, Kaixin Mansion No.107 Jinqiao Avenue, Wuhan, China
Changzhou Ruiping Chemical Co., Ltd
website:http://www.wishchem.com
Contact:+86-519-82324280
Address:No.288-1 Huacheng Road, Jintan
Contact:+86-0760-85282375
Address:zhongjing road,zhongshan torch hi-tech industrial development zone
Nanjing Qirui Material Co., Ltd.
Contact:+86-25-52320053
Address:F4-5, #17 Building, Chuang Yi Yuan, No.6 Guanghua East Street, Nanjing, 210007 P.R.China
Contact:+86-20-62802632;62802633
Address:Room 330 GIGCAS Building,No.511 Kehua Street,Tianhe District
Doi:10.1039/b208107e
(2003)Doi:10.1021/ja005785n
(2001)Doi:10.1081/SCC-100000210
(2001)Doi:10.1016/j.tet.2012.06.071
(2012)Doi:10.1016/S0022-328X(00)00552-0
(2001)Doi:10.1021/ja021146w
(2003)