Synthesis and in-vitro cytotoxic activity of novel benzo[b]phenazine-6,11- dioneand 1,4-naphthoquinone derivatives

Abstract

5,12-Dihydrobenzophenazine-6,11-diones,2-Arylamino-3-chloro-1, 4-naphthoquinones and 6,11-dihydrobenzo[b]phenazine-6,11-diones, were synthesized from 2,3-dichloro-1,4-naphthoquinone and arylamines/ phenylenediamines. Studying the cytotoxicity using EAC and human cell lines revealed that 5,12-dihydrobenzo[b]phenazine-6,11-dione (3) and 3-chloro-2-(2-pyridylamino)-1,4-naphthoquinone (10) showed selective cytotoxicity against the human lung carcinoma cell line (H460) superior to doxorubicin. Compound 3 (16.25 uM) was 1.3 times higher than that of doxorubicin. However, IC50 value of compound 10 was 9.90 uM which was 2 times higher than that (20.10 uM) of doxorubicin. These compounds were inactive against liver carcinoma (HEPG2), brain tumor (U251), cervix carcinoma (HELA) and breast carcinoma (MCF7) cell lines.