Synthesis and biological evaluation of 2,4-diaminoquinazoline derivatives as novel heat shock protein 90 inhibitors
| Autor: | Dhanaji Achyutrao Thorat, Seon Hee Seo, Tae-Joon Hong, Yong Seo Cho, Ji-Sook Hahn, Ae Nim Pae, Munikumar Reddy Doddareddy |
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| Rok vydání: | 2010 |
| Předmět: |
Clinical Biochemistry
Drug Evaluation Preclinical Pharmaceutical Science Biochemistry Heat shock protein Cell Line Tumor Drug Discovery Humans HSP90 Heat-Shock Proteins skin and connective tissue diseases Molecular Biology Cell Proliferation chemistry.chemical_classification biology Chemistry Organic Chemistry Biological activity Hsp90 Hsp70 Enzyme Enzyme inhibitor Chaperone (protein) biology.protein Quinazolines Molecular Medicine Signal transduction |
| Zdroj: | Bioorganicmedicinal chemistry letters. 21(6) |
| ISSN: | 1464-3405 |
| Popis: | Novel 2,4-diaminoquinazoline derivatives originating from a virtual screening approach were designed, synthesized and their biological activities as heat shock protein 90 (Hsp90) inhibitors were evaluated. The prepared compounds exhibited significant anti-proliferative activities against DU-145, HT-29, HCT-116, A375P and MCF-7 cancer cell lines. The selected compounds were tested against Her2, a client protein of Hsp90, and showed significant reduction in Her2 protein expression. Compound 6b was found the most potent, reduced Her2 protein expression levels and induced Hsp70 protein expression levels significantly. |
| Databáze: | OpenAIRE |
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