Design,Synthesis, and Cytotoxic Activity of Novel Natural Arylsulfonamide-Inspired Molecules |
| |
| Authors: | Wenbo Huang Liqiao Shi Manli Liu Zhigang Zhang Fang Liu Tong Long Shaohua Wen Daye Huang Kaimei Wang Ronghua Zhou Wei Fang Hongtao Hu Shaoyong Ke |
| |
| Institution: | 1.Key Laboratory of Microbial Pesticides, Ministry of Agriculture and Rural Affairs, Wuhan 430064, China; (W.H.); (L.S.); (M.L.); (Z.Z.); (F.L.); (T.L.); (S.W.); (D.H.); (K.W.); (R.Z.);2.National Biopesticide Engineering Research Centre, Hubei Biopesticide Engineering Research Centre, Hubei Academy of Agricultural Sciences, Wuhan 430064, China |
| |
| Abstract: | 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 μg/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. |
| |
| Keywords: | natural arylsulfonamides derivatives synthesis biological evaluation SARs |
|
|
