Biological evaluation of KRIBB3 analogs as a microtubule polymerization inhibitor

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 3, 2011, Pages 977-979

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

^a Korea Research Institute of Bioscience and Biotechnology (KRIBB)   (South Korea)

^b Chonnam National University   (South Korea)

Author keywords

Anti mitotic; Cancer; Inhibition; Isoxazole; Microtubule

Indexed keywords

ANTIMITOTIC AGENT; HYDROGEN; ISOXAZOLE DERIVATIVE; KRIBB3 DERIVATIVE; PHENOL; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG STRUCTURE; DRUG SYNTHESIS; MICROTUBULE ASSEMBLY; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

ANISOLES; HUMANS; ISOXAZOLES; POLYMERIZATION; STRUCTURE-ACTIVITY RELATIONSHIP; TUBULIN; TUBULIN MODULATORS;

EID: 78751645942     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.12.044     Document Type: Article

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12. 2, 0.5 mM EGTA, 1.0 mM GTP, pH 6.9) plus 5% glycerol in the 0.1% DMSO or test compounds at 4 °C. Then the sample mixture was transferred to the pre-warmed 96-well plate, and polymerization of tubulin was measured by the change in absorbance at 340 nm every 1 min for 70 min (Wallac victor2; PerkinElmer, Inc., Wellesley, MA) at 37 °C. Inhibitory activity of KRIBB3 or its analogs was calculated using initial polymerization activity (from 0 to 10 min). To compare each compound's inhibitory activity, we used initial polymerization reaction slop (from 0 to 10 min). Slop of polymerization reaction was calculated using linear equation method with Sigma Plot Program and slop of DMSO treated reaction was used as a control. Relative inhibition of tube formation is percentage of slop for KRIBB3 analogs compared to the slop for DMSO treated reaction.