Abstract
Two novel series of quinazolinone-based hybrids, including quinazolinone-1,3,4-oxadiazoles (10a–l) and quinazolinone-1,3,4-oxadiazole-benzimidazoles (8a–e), were designed and synthesized and their cytotoxic activities against three human cancer cell lines, lung cancer (A549), cervical cancer (HeLa), and breast cancer (MCF-7), were evaluated. The cytotoxic assays revealed that 10i with a lipophilic 4-fluoro-phenyl moiety at the C-2 position of the quinazolinone ring displayed good cytotoxicities against the A549 and MCF-7 cell lines, while 8b–d with the thioether-linked benzimidazole moiety incorporated on the right side of the oxadiazole ring induced comparable stronger activities toward the MCF-7 cell line, relative to the simple two-heterocycle-containing hybrid 10i. These novel quinazolinone-based hybrids could be considered as lead compounds that merit further optimization and development as anti-cancer agents.
Original language | English |
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Pages (from-to) | 61-67 |
Number of pages | 7 |
Journal | Chemical and Pharmaceutical Bulletin |
Volume | 72 |
Issue number | 1 |
DOIs | |
State | Published - 2024/01/20 |
Keywords
- 1
- 3
- 4-oxadiazole
- benzimidazole
- cytotoxicity
- hybrid structure
- quinazolinone
ASJC Scopus subject areas
- General Chemistry
- Drug Discovery