Novel hybrid nocodazole analogues as tubulin polymerization inhibitors and their antiproliferative activity
| Autor: | Ernest Hamel, Sangram S. Kale, Gangadhar J. Sanjayan, Ganesh S. Jedhe, Manas Kumar Santra, Sachin N. Meshram |
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| Rok vydání: | 2015 |
| Předmět: |
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Molecular Stereochemistry Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry Article Polymerization Tubulin binding Structure-Activity Relationship chemistry.chemical_compound Tubulin Cell Line Tumor Drug Discovery Thiophene Humans Moiety Structure–activity relationship Molecular Biology Cell Proliferation Combretastatin Dose-Response Relationship Drug Molecular Structure biology Nocodazole Organic Chemistry chemistry biology.protein Molecular Medicine Drug Screening Assays Antitumor |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 25:1982-1985 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2015.03.019 |
| Popis: | We describe the design, synthesis and SAR profiling of a series of novel combretastatin–nocodazole conjugates as potential anticancer agents. The thiophene ring in the nocodazole moiety was replaced by a substituted phenyl ring from the combretastatin moiety to design novel hybrid analogues. The hydroxyl group at the ortho position in compounds 2, 3 and 4 was used as the conformationally locking tool by anticipated six-membered hydrogen bonding. The bioactivity profiles of all compounds as tubulin polymerization inhibitors and as antiproliferative agents against the A-549 human lung cancer cell line were investigated Compounds 1 and 4 showed μM IC50 values in both assays. |
| Databáze: | OpenAIRE |
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