%0 Journal Article
%T Investigating the Anticancer Activity of Isatin/Dihydropyrazole Hybrids
%J -
%D 2019
%R https://doi.org/10.1021/acsmedchemlett.8b00596
%X A series of isatin¨Cdihydropyrazole hybrids have been synthesized in order to assess their potential as anticancer agents. In particular, 12 compounds were evaluated for their antiproliferative activity toward A549, IGR39, U87, MDA-MB-231, MCF-7, BT474, BxPC-3, SKOV-3, and H1299 cell lines, and human foreskin fibroblasts. Four compounds exhibited interesting antiproliferative activity and were further examined to determine their EC50 values toward a panel of selected tumor cell lines. The best compounds were then investigated for their induced mechanism of cell death. Preliminary structure¨Cactivity relationship indicates that the presence of a substituent such as a chlorine atom or a methyl moiety in position 5 of the isatin nucleus is beneficial for the antitumor activity. EMAC4001 proved the most promising compound within the studied series with EC50 values ranging from 0.01 to 0.38 ¦ÌM
%U https://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00596