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

doi:10.1016/j.bmcl.2018.10.020

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 journal › Article › peer-review

21 Scopus citations

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 language	English (US)
Pages (from-to)	3736-3740
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	28
Issue number	23-24
DOIs	https://doi.org/10.1016/j.bmcl.2018.10.020
State	Published - Dec 15 2018

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

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10.1016/j.bmcl.2018.10.020

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title = "Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy",

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.",

keywords = "Aminopyrazole, Cyclin dependent kinase 2, Cyclin dependent kinase 5, Growth inhibition",

author = "Sandeep Rana and Sonawane, {Yogesh A.} and Taylor, {Margaret A.} and Smitha Kizhake and Muhammad Zahid and Amarnath Natarajan",

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AU - Rana, Sandeep

AU - Sonawane, Yogesh A.

AU - Taylor, Margaret A.

AU - Kizhake, Smitha

AU - Zahid, Muhammad

AU - Natarajan, Amarnath

PY - 2018/12/15

Y1 - 2018/12/15

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AB - 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.

KW - Aminopyrazole

KW - Cyclin dependent kinase 2

KW - Cyclin dependent kinase 5

KW - Growth inhibition

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IS - 23-24

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

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