Synthesis of novel triazole/isoxazole functionalized 7-(trifluoromethyl)pyrido[2,3-d]pyrimidine derivatives as promising anticancer and antibacterial agents.

Abstract

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.

• Authors: R Naresh Kumar, G Jitender Dev, N Ravikumar, D Krishna Swaroop, B Debanjan, G Bharath, B Narsaiah, S Nishant Jain, A Gangagni Rao
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 26 Issue 12 Pg. 2927-2930 (06 15 2016) ISSN: 1464-3405 [Electronic] England
• PMID: 27130357 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2016 Elsevier Ltd. All rights reserved.

Chemical References

• Anti-Bacterial Agents
• Antineoplastic Agents
• Isoxazoles
• Triazoles

Topics

• Anti-Bacterial Agents (chemical synthesis, chemistry, pharmacology)
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Dose-Response Relationship, Drug
• Drug Screening Assays, Antitumor
• Gram-Negative Bacteria (drug effects)
• Gram-Positive Bacteria (drug effects)
• Humans
• Isoxazoles (chemical synthesis, chemistry, pharmacology)
• Microbial Sensitivity Tests
• Molecular Structure
• Structure-Activity Relationship
• Triazoles (chemical synthesis, chemistry, pharmacology)