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

• Authors: Marwa Ahmed , Naja Magdy
• Languages of publication: EN

Abstracts

EN

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.

Keywords

EN

cytotoxicity; MCF-7; quinazoline; CASP3

• Journal: Acta Poloniae Pharmaceutica - Drug Research
• Year: 2018
• Volume: 75
• Issue: 6
• Pages: 1321-1328

Dates

published

2018-12-31

Contributors

author

Marwa Ahmed

author

Naja Magdy

Identifiers

DOI

10.32383/appdr/89488