Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors

Jinho Lee; Hwangeun Choi; Kyoung-Hee Kim; Shinwu Jeong; Jong-Wook Park; Chul-Su Baek; Sei-Hee Lee

doi:10.1016/j.bmcl.2008.03.002

Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2292-5. doi: 10.1016/j.bmcl.2008.03.002. Epub 2008 Mar 6.

Authors

Jinho Lee¹, Hwangeun Choi, Kyoung-Hee Kim, Shinwu Jeong, Jong-Wook Park, Chul-Su Baek, Sei-Hee Lee

Affiliation

¹ Department of Chemistry, Keimyung University, 1000 Sindang-Dong, Dalseo-Gu, Daegu 704-701, South Korea. jinho@kmu.ac.kr

PMID: 18353638
DOI: 10.1016/j.bmcl.2008.03.002

Abstract

A novel series of 3,5-diaminoindazoles were prepared and found to be CDK inhibitors. Potent inhibitors against CDK1 and CDK2 were obtained by introduction of 1lambda(6)-isothiazolidine-1,1-dioxide at 5-position of indazole. Anti-proliferative activities of compounds were evaluated using EJ, HCT116, SW620, and A549 cancer cell lines.

Publication types

Evaluation Study
Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Cyclin-Dependent Kinases / antagonists & inhibitors*
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacology
Humans
Imidazoles / chemical synthesis
Imidazoles / pharmacology*
Inhibitory Concentration 50
Models, Chemical
Structure-Activity Relationship

Substances

Antineoplastic Agents
Enzyme Inhibitors
Imidazoles
Cyclin-Dependent Kinases

Associated data

PDB/2R64