Title of article :
DESIGN AND SYNTHESIS OF NEW EGFR- TYROSINE KINASE INHIBITORS CONTAINING PYRAZOLO[3,4-d]PYRIMIDINE CORES AS ANTICANCER AGENTS
Author/Authors :
Bakr, Rania B. Beni-Suef University - Faculty of Pharmacy - Department of Pharmacutical Organic Chemistry, Egypt , Abdelall, Eman K. A. Beni-Suef University - Faculty of Pharmacy - Department of Pharmacutical Organic Chemistry, Egypt , Abdel-Hamid, Mohamed K. Cairo University - Faculty of Pharmacy - Department of Organic Chemistry, Egypt , Kandeel, Manal M. Cairo University - Faculty of Pharmacy - Department of Organic Chemistry, Egypt
Abstract :
New designed EGFR inhibitors (7-11) were prepared from the pyrazolo[3,4-d]pyrimidine intermediates 4a-d including different moieties. All newly synthesized compounds were confirmed by elemental analyses and spectral data. The molecular simulation docking to protein tyrosine kinase (EGFR), using erlotinib (Tarceva TM) as a lead compound was also studied. Some of the prepared compounds were screened for in-vitro cytotoxic activity. The docking results were in coincidence with the biological results that indicated compound 7a showed an inhibitory activity against human breast carcinoma cell line (MCF-7) [IC50 (14.86μM)].
Journal title :
Bulletin Of Pharmaceutical Sciences, Assiut University
Journal title :
Bulletin Of Pharmaceutical Sciences, Assiut University
