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Novel series of 4-substituted 6,8-dibromo-2-(4-chlorophenyl)-quinazoline have been designed and synthesized. All new derivatives were tested in vitro against MCF-7. Compounds VIc and VIIb exerted powerful cytotoxic activity with low IC50 (6.3 and 6.9 mu M) compared to doxorubicin 7.72 mu M. Compounds VIa, Vb and Vc showed moderate cytotoxic effects with IC50 range (10.0 - 16.7) mu M, respectively. Compounds Va, VIIc, VIIa, IVb, IVc, VIb and IVa showed promising cytotoxic effects with IC50 range (20.3 - 40 mu M, respectively.). Exploring their apoptotic effect; all compounds activated apoptotic cascade in MCF-7. Compounds VIc and VIIb increased CASP3 activity more than doxorubicin.

DESIGN, SYNTHESIS AND ANTICANCER ACTIVITY EVALUATION OF NEW QUINAZOLINE DERIVATIVES LINKED TO THIAZOLIDINONE, AZETIDINONE OR OXADIAZOL MOIETIES