2. Academic Validation
  3. Synthesis of novel 1,2,3-triazole tagged pyrazolo[3,4-b]pyridine derivatives and their cytotoxic activity

Synthesis of novel 1,2,3-triazole tagged pyrazolo[3,4-b]pyridine derivatives and their cytotoxic activity

  • Bioorg Med Chem Lett. 2014 Feb 1;24(3):746-9. doi: 10.1016/j.bmcl.2013.12.107.
Chavva Kurumurthy 1,  Banda Veeraswamy 1,  Pillalamarri Sambasiva Rao 1,  Gautham Santhosh Kumar 1,  Pamulaparthy Shanthan Rao 1,  Velaturu Loka Reddy 2,  Janapala Venkateswara Rao 2,  Banda Narsaiah 3
Affiliations

Affiliations

  • 1 Fluoro Organic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 607, India.
  • 2 Biology division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India.
  • 3 Fluoro Organic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 607, India. Electronic address: narsaiah@iict.res.in.
PMID: 24424132 DOI: 10.1016/j.bmcl.2013.12.107
Abstract

A series of novel 1,2,3-triazole tagged pyrazolo[3,4-b]pyridine derivatives 3 and 4 were prepared respectively starting from 6-phenyl-4-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridin-3-amine 1 via selective N-propargylation, followed by reaction with diverse substituted alkyl/perfluoroalkyl/aryl/aryl amide azides under Sharpless conditions. All the synthesized compounds 3 and 4 were screened for cytotoxic activity against four human Cancer cell lines such as U937, THP-1, HL60 and B16-F10. Compounds 3e, 4g, 4i and 4j which showed promising activity have been identified.

Keywords

1,2,3-Triazoles; Cytotoxic activity; Propargylation; Pyrazolo[3,4-b]pyridine; Sharpless conditions.

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