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Synthesis, Cytotoxic, and Antibacterial Evaluation of Quinazolinone Derivatives with Substituted Amino Moiety
Author(s) -
Zhan Xiaoping,
Xu Yun,
Qi Qi,
Wang Yaolin,
Shi Huiying,
Mao Zhenmin
Publication year - 2018
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201700513
Subject(s) - quinazolinone , chemistry , moiety , cytotoxicity , cytotoxic t cell , antibacterial activity , escherichia coli , mtt assay , stereochemistry , combinatorial chemistry , cell culture , cancer cell lines , bacteria , biochemistry , cell growth , cancer cell , in vitro , cancer , biology , gene , genetics
A series of novel quinazolinone derivatives containing a substituted amino moiety were synthesized, evaluated for their cytotoxic and antibacterial activities. The results of MTT assay showed that all synthesized target compounds 5A – 5O showed potent cytotoxicity against SGC ‐7901 ( IC 50 , 0.72 – 1.41 μ m ). Moreover, the compounds 5D , 5I , and 5K showed better selectivity as compared with positive controls pemetrexed and MTX due to weak cytotoxicity against normal tissue cell line HUVSMC . Among synthesized compounds, the compounds 5E , 5J , 5L , and 5N showed broad‐spectrum cytotoxic activities against at least four cancer cell lines at a micromolar level. The results of antibacteria evaluation revealed that all synthesized compounds showed good to moderate antibacterial activities against Gram ‐negative bacteria Escherichia coli . Among them, the MIC values of the compounds 5C , 5F , and 5M were 0.31 μg/ mL .