Syntheses and Cytotoxicities of Quinazolinone-Based Conjugates

Hieu Trong Le, Kiep Minh Do, Quy Phu Nguyen, Chau Nguyen Minh Doan, Nhi Ai Nguyen, Tai Thi Phan, Xuyen Thi Cam Tran, Quy Thi Kim Ha, De Quang Tran, Hiroyuki Morita, Hue Thi Buu Bui*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

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 languageEnglish
Pages (from-to)61-67
Number of pages7
JournalChemical and Pharmaceutical Bulletin
Volume72
Issue number1
DOIs
StatePublished - 2024/01/20

Keywords

  • 1
  • 3
  • 4-oxadiazole
  • benzimidazole
  • cytotoxicity
  • hybrid structure
  • quinazolinone

ASJC Scopus subject areas

  • General Chemistry
  • Drug Discovery

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