DESIGN AND SYNTHESIS OF NEW EGFR- TYROSINE KINASE INHIBITORS CONTAINING PYRAZOLO[3,4-d]PYRIMIDINE CORES AS ANTICANCER AGENTS
Bakr, R., Abdelall, E., Abdel-Hamid, M., Kandeel, M. (2012). DESIGN AND SYNTHESIS OF NEW EGFR- TYROSINE KINASE INHIBITORS CONTAINING PYRAZOLO[3,4-d]PYRIMIDINE CORES AS ANTICANCER AGENTS. EKB Journal Management System, 35(1), 27-42. doi: 10.21608/bfsa.2012.64596
Rania B. Bakr; Eman K. A. Abdelall; Mohamed K. Abdel-Hamid; Manal M. Kandeel. "DESIGN AND SYNTHESIS OF NEW EGFR- TYROSINE KINASE INHIBITORS CONTAINING PYRAZOLO[3,4-d]PYRIMIDINE CORES AS ANTICANCER AGENTS". EKB Journal Management System, 35, 1, 2012, 27-42. doi: 10.21608/bfsa.2012.64596
Bakr, R., Abdelall, E., Abdel-Hamid, M., Kandeel, M. (2012). 'DESIGN AND SYNTHESIS OF NEW EGFR- TYROSINE KINASE INHIBITORS CONTAINING PYRAZOLO[3,4-d]PYRIMIDINE CORES AS ANTICANCER AGENTS', EKB Journal Management System, 35(1), pp. 27-42. doi: 10.21608/bfsa.2012.64596
Bakr, R., Abdelall, E., Abdel-Hamid, M., Kandeel, M. DESIGN AND SYNTHESIS OF NEW EGFR- TYROSINE KINASE INHIBITORS CONTAINING PYRAZOLO[3,4-d]PYRIMIDINE CORES AS ANTICANCER AGENTS. EKB Journal Management System, 2012; 35(1): 27-42. doi: 10.21608/bfsa.2012.64596

DESIGN AND SYNTHESIS OF NEW EGFR- TYROSINE KINASE INHIBITORS CONTAINING PYRAZOLO[3,4-d]PYRIMIDINE CORES AS ANTICANCER AGENTS

Bulletin of Pharmaceutical Sciences Assiut University
Article 3, Volume 35, Issue 1, June 2012, Page 27-42  XML PDF (590.44 K)
Document Type: Original Article
DOI: 10.21608/bfsa.2012.64596
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Authors
Rania B. Bakr1; Eman K. A. Abdelall* 1; Mohamed K. Abdel-Hamid2; Manal M. Kandeel2
1Department of Pharmacutical Organic Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt
2Department of Organic Chemistry, Faculty of Pharmacy, Cairo University Cairo, 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)].
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