SYNTHESIS AND IN-VITRO CYTOTOXIC ACTIVITY OF NOVEL BENZO[b]PHENAZINE-6,11-DIONE AND 1,4- NAPHTHOQUINONE DERIVATIVES

Document Type : Original Article

Authors

1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Nasr City, Cairo, Egypt

2 Department of Radiation Biology, Natural Center for Radiation Research and Technology, Atomic Energy Authority, Cairo, Egypt

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.

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