Rakesh Ponaganti*, N. Kanaka Chari and B. Shailendra

Author(s): SYNTHESIS AND EVALUATION OF NITROGEN ANALOGUES OF FLAVANONES-TETRAHYDROQUINOLONES AS CYTOTOXIC AGENTS

Abstract: Studies by Kellies and Vickery1 showed that several naturally occurring and synthetic flavonoids were found to inhibit aromatase. The present investigation includes synthesis and evaluation of novel tetrahydroquinolones (nitrogen analogues of flavanones) for their cytotoxic activity on hormone dependent human cancer cell lines including breast (MCF-7), ovarian (OVC-AR) and prostate (DU-145). The compounds synthesized (7a-j) showed potent cytotoxic effects in micromolar range. Among the compounds tested 7d & 7j exhibited good cytotoxic activites with IC50 values of 4 & 3 μM against MCF-7 and 7 & 3 μM against OVC-AR and 11 & 8 μM against DU-105 cell lines respectively.

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