3-Hydroxychromones as cyclin-dependent kinase inhibitors: synthesis and biological evaluation

Jinho Lee; Taesik Park; Shinwu Jeong; Kyoung-Hee Kim; Changyong Hong

doi:10.1016/j.bmcl.2006.12.011

3-Hydroxychromones as cyclin-dependent kinase inhibitors: synthesis and biological evaluation

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1284-7. doi: 10.1016/j.bmcl.2006.12.011. Epub 2006 Dec 15.

Authors

Jinho Lee¹, Taesik Park, Shinwu Jeong, Kyoung-Hee Kim, Changyong Hong

Affiliation

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

PMID: 17178224
DOI: 10.1016/j.bmcl.2006.12.011

Abstract

A novel series of 3-hydroxychromones were prepared and found to be CDK inhibitors. Isothiazolidine 1,1-dioxide analogues showed potent CDK1 and CDK2 inhibitory activities and inhibited proliferation of EJ, HCT116, SW620, and MDAMB468 cancer cells.

MeSH terms

Antineoplastic Agents / chemistry*
Antineoplastic Agents / pharmacology
Binding Sites
Cell Line, Tumor
Cell Survival / drug effects
Chromones / chemical synthesis*
Chromones / pharmacology*
Cyclin-Dependent Kinase 2 / antagonists & inhibitors
Cyclin-Dependent Kinase Inhibitor Proteins / chemical synthesis*
Cyclin-Dependent Kinase Inhibitor Proteins / pharmacology
Humans
Inhibitory Concentration 50
Protein Binding
Structure-Activity Relationship

Substances

3-hydroxychromone
Antineoplastic Agents
Chromones
Cyclin-Dependent Kinase Inhibitor Proteins
CDK2 protein, human
Cyclin-Dependent Kinase 2