Diarylamine-Guided Carboxamide Derivatives: Synthesis, Biological Evaluation, and Potential Mechanism of Action

Diarylamines are a class of important skeleton widely existing in drugs or natural products. To discover novel diarylamine analogues as potential drugs, two series of diamide and carboxamide derivatives containing diarylamine scaffold were designed, synthesized and evaluated for their potential cyto...

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Published inFrontiers in chemistry Vol. 10; p. 953523
Main Authors Ke, Shaoyong, Huang, Wenbo, Zhang, Zhigang, Wang, Yueying, Zhang, Yani, Wu, Zhaoyuan, Fang, Wei, Wan, Zhongyi, Gong, Yan, Yang, Jingzhong, Wang, Kaimei, Shi, Liqiao
Format Journal Article
LanguageEnglish
Published Frontiers Media S.A 12.07.2022
Subjects
bioactivity
carboxamide
Chemistry
diamides
diarylamine
synthesis
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Summary:Diarylamines are a class of important skeleton widely existing in drugs or natural products. To discover novel diarylamine analogues as potential drugs, two series of diamide and carboxamide derivatives containing diarylamine scaffold were designed, synthesized and evaluated for their potential cytotoxic activities. The bioassay results indicated that some of the obtained compounds (C5, C6, C7, C11) exhibited good cytotoxic effect on cancer cell lines (SGC-7901, A875, HepG2), especially, compound C11 present significantly selective proliferation inhibition activity on cancer and normal cell lines (MARC145). In addition, the possible apoptosis induction for highly potential molecules was investigated, which present compound C11 could be used as novel lead compound for discovery of promising anticancer agents.
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This article was submitted to Medicinal and Pharmaceutical Chemistry, a section of the journal Frontiers in Chemistry
Mahmoud A. Al-Sha’er, Zarqa Private University, Jordan
Reviewed by: Alessandra Montalbano, University of Palermo, Italy
Edited by: Marco Tutone, University of Palermo, Italy
ISSN:2296-2646
2296-2646
DOI:10.3389/fchem.2022.953523