DESIGN, SYNTHESIS AND ANTICANCER ACTIVITY EVALUATION OF NEW QUINAZOLINE DERIVATIVES LINKED TO THIAZOLIDINONE, AZETIDINONE OR OXADIAZOL MOIETIES
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Novel series of 4-substituted 6,8-dibromo-2-(4-chloro-phenyl)-quinazoline have been designed and synthesized. All new derivatives were tested in vitro against MCF-7. Compounds Xc and XIb exerted powerful cytotoxic activity with low IC50 (6.3 and 6.9 µM) compared to doxorubicin 7.72 µM. Compounds Xa, IXb and IXc showed moderate cytotoxic effects with IC50 range (10.0 – 16.7) µM, respectively. Compounds IXa, XIc, XIa, VIIb, VIIIc, Xb and VIIIa showed promising cytotoxic effects with IC50 range (20.3 – 40 µM, respectively. ). Exploring their apoptotic effect; all compounds activated apoptotic cascade in MCF-7. Compounds Xc and XIb increased CASP3 activity more than doxorubicin.
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