Design and synthesis of new EGFR- tyrosine kinase inhibitors containing pyrazolo[3,4-pywmidine cores as anticancer agents
Bulletin of Pharmaceutical Sciences-Assiut University. 2012; 35 (Part 1): 27-42
em Inglês, Árabe
| IMEMR
| ID: emr-154254
ABSTRACT
New designed EGFR inhibitors [7-1 1] were prepare dfrom the pyrazolo[3t4-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] [1C so [14.86microM]
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Índice:
IMEMR (Mediterrâneo Oriental)
Assunto principal:
Pirazóis
/
Antiasmáticos
/
Antineoplásicos
Idioma:
Árabe
/
Inglês
Revista:
Bull. Pharm. Sci.-Assiut Univ.
Ano de publicação:
2012
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