Synthesis of novel triazole/isoxazole functionalized 7-(trifluoromethyl)pyrido[2,3- d ]pyrimidine derivatives as promising anticancer and antibacterial agents
| Autor: | S. Nishant Jain, D. Krishna Swaroop, G. Jitender Dev, G. Bharath, N. Ravikumar, A. Gangagni Rao, B. Debanjan, R. Naresh Kumar, Banda Narsaiah |
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| Rok vydání: | 2016 |
| Předmět: |
Pyrimidine
Stereochemistry Clinical Biochemistry Triazole Pharmaceutical Science Antineoplastic Agents Microbial Sensitivity Tests Gram-Positive Bacteria 01 natural sciences Biochemistry Structure-Activity Relationship chemistry.chemical_compound Minimum inhibitory concentration Cell Line Tumor Gram-Negative Bacteria Drug Discovery Humans Structure–activity relationship Isoxazole Molecular Biology Cell Proliferation Trifluoromethyl Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Cell growth Organic Chemistry Isoxazoles Triazoles Anti-Bacterial Agents 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry Molecular Medicine Drug Screening Assays Antitumor Antibacterial activity |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 26:2927-2930 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2016.04.038 |
| Popis: | A series of novel 1,2,3-triazole/isoxazole functionalized pyrido[2,3-d]pyrimidine derivatives 6a-c, 7a-h and 8a-e were prepared in series of synthetic steps. All the compounds screened for the anticancer activity against four human cancer cell lines using Nocodazole as standard. Compounds 7d and 7h showed highest activity against PANC-1 (pancreatic cancer) and A549 (lung cancer) cell lines respectively and more than standard. All the compounds also screened for antibacterial activity using Rifampicin and Ciprofloxacin as standards and identified promising compounds further evaluated for minimum inhibitory concentration to validate the data. |
| Databáze: | OpenAIRE |
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