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Design, synthesis and biological evaluation of some novel substituted quinazoline derivatives as antitumor agents.

100%
Ahmed M., Magdy N.
Acta Poloniae Pharmaceutica - Drug Research
|
2018
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vol. 75
|
issue 3
EN
New series of 6,8-dibromo-2-(4-chlorophenyl)quinazolin-4-yloxy derivatives were synthesized and their cytotoxic activity on MCF7, HEPG2 and HCT116 cell lines were evaluated. Compound XI and XIIIb were two times more active than doxorubicin on MCF7 cancer cell line. Compound VIIIa was 3 times more active than doxorubicin on HEPG2 cancer cell line. While compounds XII, XIIIa and XIIIb were more potent than doxorubicin on HCT116 cancer cell line. IC50 of all newly synthesized compounds were evaluated in vitro for thier inhibition to EGFR tyrosine kinase. All compound show good inhibitory activity on EGFR tyrosine kinase with IC50 range (6.19-19.87) µM.
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DESIGN, SYNTHESIS AND ANTICANCER ACTIVITY EVALUATION OF NEW QUINAZOLINE DERIVATIVES LINKED TO THIAZOLIDINONE, AZETIDINONE OR OXADIAZOL MOIETIES

100%
Ahmed M., Magdy N.
Acta Poloniae Pharmaceutica - Drug Research
|
2018
|
vol. 75
|
issue 6
1321-1328
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.
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