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Design, Synthesis, and Cytotoxic Activity of Novel Natural Arylsulfonamide-Inspired Molecules

文献类型： 外文期刊

作者： Huang, Wenbo 1 ; Shi, Liqiao 1 ; Liu, Manli 1 ; Zhang, Zhigang 1 ; Liu, Fang 1 ; Long, Tong 1 ; Wen, Shaohua 1 ; Huang, Daye 1 ; Wang, Kaimei 1 ; Zhou, Ronghua 1 ; Fang, Wei 1 ; Hu, Hongtao 1 ; Ke, Shaoyong 1 ;

作者机构： 1.Minist Agr & Rural Affairs, Key Lab Microbial Pesticides, Wuhan, Peoples R China

2.Hubei Acad Agr Sci, Natl Biopesticide Engn Res Ctr, Hubei Biopesticide Engn Res Ctr, Wuhan, Peoples R China

关键词： natural arylsulfonamides; derivatives; synthesis; biological evaluation; SARs

期刊名称：MOLECULES （ 影响因子：4.927； 五年影响因子：5.11 ）

ISSN：

年卷期： 2022 年 27 卷 5 期

页码：

收录情况： SCI

摘要： Primary arylsulfonamide functional groups feature prominently in diverse pharmaceuticals. However, natural arylsulfonamides are relatively infrequent. In this work, two novel arylsulfonamide natural products were first synthesized, and then a series of novel molecules derived from natural arylsulfonamides were designed and synthesized, and their in vitro cytotoxic activities against A875, HepG2, and MARC145 cell lines were systematically evaluated. The results indicate that some of these arylsulfonamide derivatives exhibit significantly good cytotoxic activity against the tested cell lines compared with the control 5-fluorouracil (5-FU), such as compounds 10l, 10p, 10q, and 10r. In particular, the potential molecule 10q, containing a carbazole moiety, exhibited the highest inhibitory activity against all tested cell lines, with IC50 values of 4.19 +/- 0.78, 3.55 +/- 0.63, and 2.95 +/- 0.78 mu g/mL, respectively. This will offer the potential to discover novel drug-like compounds from the sparsely populated area of natural products that can lead to effective anticancer agents.

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