Design, synthesis and biological evaluation of novel 1,5-disubstituted isatin derivatives as antitumor agents

AbstractIsatin (1H-indole-2,3-dione) was reported to possess anticancer activities through its effect on tumor proliferation, apoptosis, and metastasis in vitro and in vivo. Here, we described the synthesis of a novel series of 1,5-disubstituted isatin derivatives with 2-indolinone scaffold as antitumor agents. Most of the synthesized compounds revealed potent antiproliferative effects in mantle cell lymphoma (MCL) cell lines, among which7l possessed promising activities with IC50 values ranging from 0.4 to 1.3  μM. Following flow cytometric analysis, compound7l efficiently arrested the cell cycle at G2/M phase, and induced apoptosis. Thus, this study shows promise in therapeutics of 1,5-disubstituted isatin derivatives in MCL and provides novel potential and efficient antitumor agents.

Source: Medicinal Chemistry Research - October 7, 2020 Category: Chemistry Source Type: research