In the quest for novel effective carbonic anhydrase inhibitors, some sulfonamide derivatives of pyridyl-indole based chalcone were synthesized and screened in vitro for inhibitory activity against human carbonic anhydrase IX isoform. Among all the synthesized compounds (SC2 -SC11), only three compounds SC3, SC7 and SC10 were found to have better binding affinity as shown by molecular docking and fluorescence binding studies. Further, the enzyme inhibition assay and in vitro anti-tumor evaluation against MCF-7 and HepG-2 cell lines revealed that the compounds SC3, SC7 and SC10 inhibited the CA IX selectively, possessed predominant anti-proliferative potential and significantly induced apoptosis in cancerous cells.

为了寻求新型有效的碳酸酐酶抑制剂，合成了吡啶基-吲哚基查尔酮的一些磺酰胺衍生物，并在体外筛选了对人碳酸酐酶IX同工型的抑制活性。如分子对接和荧光结合研究所示，在所有合成的化合物（SC2-SC11）中，仅发现三种化合物SC3，SC7和SC10具有更好的结合亲和力。此外，针对MCF-7和HepG-2细胞系的酶抑制试验和体外抗肿瘤评估表明，化合物SC3，SC7和SC10选择性抑制CA IX，具有主要的抗增殖潜力，并能显着诱导癌细胞的凋亡细胞。