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)].
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. Bulletin of Pharmaceutical Sciences Assiut University, 35(1), 27-42. doi: 10.21608/bfsa.2012.64596
MLA
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". Bulletin of Pharmaceutical Sciences Assiut University, 35, 1, 2012, 27-42. doi: 10.21608/bfsa.2012.64596
HARVARD
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', Bulletin of Pharmaceutical Sciences Assiut University, 35(1), pp. 27-42. doi: 10.21608/bfsa.2012.64596
VANCOUVER
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. Bulletin of Pharmaceutical Sciences Assiut University, 2012; 35(1): 27-42. doi: 10.21608/bfsa.2012.64596
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