Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy

Sandeep Rana, Yogesh A. Sonawane, Margaret A. Taylor, Smitha Kizhake, Muhammad Zahid, Amarnath Natarajan

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

We synthesized a library of aminopyrazole analogs to systematically explore the hydrophobic pocket adjacent to the hinge region and the solvent exposed region of cyclin dependent kinases. Structure-activity relationship studies identified an optimal substitution for the hydrophobic pocket and analog 24 as a potent and selective CDK2/5 inhibitor.

Original languageEnglish (US)
Pages (from-to)3736-3740
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume28
Issue number23-24
DOIs
StatePublished - Dec 15 2018

Fingerprint

Cyclin-Dependent Kinases
Hinges
Structure-Activity Relationship
Libraries
Substitution reactions
Neoplasms
Therapeutics

Keywords

  • Aminopyrazole
  • Cyclin dependent kinase 2
  • Cyclin dependent kinase 5
  • Growth inhibition

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy. / Rana, Sandeep; Sonawane, Yogesh A.; Taylor, Margaret A.; Kizhake, Smitha; Zahid, Muhammad; Natarajan, Amarnath.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 28, No. 23-24, 15.12.2018, p. 3736-3740.

Research output: Contribution to journalArticle

Rana, Sandeep ; Sonawane, Yogesh A. ; Taylor, Margaret A. ; Kizhake, Smitha ; Zahid, Muhammad ; Natarajan, Amarnath. / Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy. In: Bioorganic and Medicinal Chemistry Letters. 2018 ; Vol. 28, No. 23-24. pp. 3736-3740.
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