ABSTRACT
Objective·To discover lead compounds with 6,11-dihydro-5H-benzo[a]carbazole as core scaffold that can inhibit the proliferation of cervical cancer cells. Methods?·?A series of 6,11-dihydro-5H-benzo[a]carbazole derivatives and analogs were synthesized using Fischer indole synthesis method, and their anticancer activity against HeLa cells was tested in vitro by CCK8 test. Results?·?2-Methoxy-6,11-dihydro-5H-benzo[a]carbazole and 8-chloro-2-methoxy-6,11-dihydro-5H-benzo[a]carbazole could significantly inhibit the proliferation of HeLa cells with the half maximal inhibitory concentration ( IC50) values of 9.61?μmol/L and 16.52?μmol/L, respectively. Conclusion?·?Two objective lead compounds were found. Among 6,11-dihydro-5H-benzo[a]carbazole derivatives, compounds with methoxy group at the C-2 position of the core scaffold show better activity against proliferation of cervical cancer cells.
ABSTRACT
Objective·To discover and develop novel monoacylglycerol lipase (MAGL) inhibitors.Methods·Computational screening,rational structure analysis and biological assessment was used.Results·A series of natural flavonoid MAGL inhibitors were identified.Compound 9 (quercetin) presented the highest activity with an IC50 value of 36 μmol/L.Conclusion·Several natural flavonoid MAGL inhibitors were identified,which are expected to bring novel hits for discovery ofMAGL inhibitors.