Drug Res (Stuttg) 2013; 63(03): 129-136
DOI: 10.1055/s-0032-1333306
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Synthesis, and Docking Studies of Some Fused-quinazolines and Quinazolines Carrying Biological Active Isatin Moiety as Cell-cycle Inhibitors of Breast Cancer Cell Lines

A. A. Radwan
1   kayyali Chair, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
2   Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
F. K. Alanazi
1   kayyali Chair, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
A. Al-Dhfyan
3   Stem Cell Therapy Program, King Faisal Specialized Hospital and Research Center, Riyadh, Saudi Arabia
› Author Affiliations
Further Information

Publication History

received 06 November 2012

accepted 31 December 2012

Publication Date:
26 February 2013 (online)


3 series of novel fused heterocyclic systems, viz. triazolo[4,3-a]quinazolin-7-ones (3), [1] [2] [4] [5]-tetrazino[4,3-a]-quinazolin-8-ones (5) and Schiff’s bases of isatin derivatives with 2-hydrazinoquinazolin-4-ones (7) have been synthesized. Several of them showed variable and promising in vitro antiproliferative activity against the MCF-7 cells. Compounds 3a-3c, 6, 7a-7 f showed promising activity (IC50=12.45–15.79 μM). Compound 7 f possessed notable cell cycle disrupting and apoptotic activities with enhanced selectivity against cancer cells, suggesting the potential for the development of new selective cell cycle inhibitors. In silico docking study of the compound 7 f with EGFR enzyme postulated that the designed compound might act on the same enzyme target where DJK_3021_A x-ray structure acted.

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