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

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

  • Bioorg Med Chem Lett. 2016 Jun 15;26(12):2927-2930. doi: 10.1016/j.bmcl.2016.04.038.
R Naresh Kumar 1,  G Jitender Dev 1,  N Ravikumar 2,  D Krishna Swaroop 1,  B Debanjan 3,  G Bharath 4,  B Narsaiah 5,  S Nishant Jain 3,  A Gangagni Rao 4
Affiliations

Affiliations

  • 1 Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India; Academy of Scientific and Innovative Research, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 2 Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 3 Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 4 Bioengineering & Environmental Science, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 5 Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India; Academy of Scientific and Innovative Research, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India. Electronic address: narsaiah@iict.res.in.
PMID: 27130357 DOI: 10.1016/j.bmcl.2016.04.038
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.

Keywords

1,3-Dipolar cycloaddition; Anticancer; Isoxazole; Pyrido[2,3-d]pyrimidine; Sharpless conditions; Triazole.

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