Document Details

Document Type : Article In Journal 
Document Title :
Single step synthesis of new fused pyrimidine derivatives and their evaluation as potent Aurora-A kinase inhibitors
Single step synthesis of new fused pyrimidine derivatives and their evaluation as potent Aurora-A kinase inhibitors
 
Subject : Chemistry 
Document Language : English 
Abstract : A simple, facile, efficient and one pot three-component procedure for the synthesis of pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and pyrimido[1,2-a]benzimidazoles ring systems incorporating phenylsulfonyl moiety was developed via the reaction of 1-aryl-2-(phenylsulfonyl)ethanone derivatives 1a-d with the appropriate heterocyclic amine and triethyl orthoformate and evaluated as Aurora-A kinase inhibitors. The cytotoxic activity of the newly synthesized compounds against HST116 colon tumor cell line was investigated. 2,7-Diphenyl-6-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine (4b) and its p-methoxy analogue 4c were found to be equipotent to Doxorubicin as a reference drug. Molecular modeling study was carried out in order to rationalize the in vitro anti-tumor results. 
ISSN : 0223-5234 
Journal Name : European Journal of Medicinal Chemistry 
Volume : 46 
Issue Number : 9 
Publishing Year : 1432 AH
2011 AD 
Article Type : Article 
Added Date : Monday, April 30, 2012 

Researchers

Researcher Name (Arabic)Researcher Name (English)Researcher TypeDr GradeEmail
Mohamed R ShaabanShaaban, Mohamed RResearcherDoctorate 
ثامر صالحSaleh, Tamer SResearcherDoctoratetamsaid@yahoo.com
Abdelrahman S MayhoubMayhoub, Abdelrahman SResearcherDoctorate 
Ahmad M FaragFarag, Ahmad MResearcherDoctorate 

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