Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer

In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (5a–e and 7a–i) was designed synthesised. The anticancer activity for compounds (5b–d, 7a, 7b, 7d 7g) measured against NCI-55 human cancer cell lines. Compound 5d most efficient, thus subjected to five-dose screen where it showed excellent broad almost all tested subpanels. Furthermore, good anti-proliferative towards colorectal SW-620 HT-29 lines, with an inhibitory effect 5a (IC50 = 8.7 9.4 µM (5a), 6.5 9.8 (5d), respectively). Both displayed selective cytotoxicity safety profile. addition, both provoked apoptosis in dose dependent manner cells. Also, they significantly inhibited anti-apoptotic Bcl2 protein expression increased cleaved PARP level that resulted cells apoptosis.