Biological evaluation of KRIBB3 analogs as a microtubule polymerization inhibitor

Sangku Lee; Jae Nyoung Kim; Hyeong Kyu Lee; Kab Seog Yoon; Ki Deok Shin; Byoung-Mog Kwon; Dong Cho Han

doi:10.1016/j.bmcl.2010.12.044

Biological evaluation of KRIBB3 analogs as a microtubule polymerization inhibitor

Bioorg Med Chem Lett. 2011 Feb 1;21(3):977-9. doi: 10.1016/j.bmcl.2010.12.044. Epub 2010 Dec 13.

Authors

Sangku Lee¹, Jae Nyoung Kim, Hyeong Kyu Lee, Kab Seog Yoon, Ki Deok Shin, Byoung-Mog Kwon, Dong Cho Han

Affiliation

¹ Bio-Therapeutics Research Institute, KRIBB, Ochang, Republic of Korea. sangku@kribb.re.kr

PMID: 21215627
DOI: 10.1016/j.bmcl.2010.12.044

Abstract

A series of KRIBB3 analogs were synthesized by modifying substituents at aryl moieties of KRIBB3 for examining structure-activity relationships, and their inhibitory activities on microtubule polymerization were evaluated. The presence of free phenolic hydrogens in aryl moieties of KRIBB3 analogs plays an important role in inhibition of microtubule polymerization.

Publication types

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

MeSH terms

Anisoles / chemical synthesis
Anisoles / chemistry*
Anisoles / pharmacology
Humans
Isoxazoles / chemical synthesis
Isoxazoles / chemistry*
Isoxazoles / pharmacology
Polymerization
Structure-Activity Relationship
Tubulin / chemistry*
Tubulin / metabolism
Tubulin Modulators / chemical synthesis
Tubulin Modulators / chemistry*
Tubulin Modulators / pharmacology

Substances

5-(5-ethyl-2-hydroxy-4-methoxyphenyl)-4-(4-methoxyphenyl)isoxazole
Anisoles
Isoxazoles
Tubulin
Tubulin Modulators