1. 2-(6-Aryl-3(Z)-hexen-1,5-diynyl)anilines as a New Class of Potent Antitubulin Agents
- Author
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Ying-Ting Lin, Shinne-Ren Lin, Ching-Chih Lin, Chi-Fong Lin, Yu-Hsiang Lo, Hong Yi-Ren, Tsai-Hui Duh, Sheng-Huei Yang, Shyh-Chyun Yang, Long-Sen Chang, and Ming-Jung Wu
- Subjects
Stereochemistry ,Microtubules ,Chemical synthesis ,Structure-Activity Relationship ,chemistry.chemical_compound ,Biopolymers ,Tubulin ,Cell Line, Tumor ,Drug Discovery ,Humans ,Caspase ,Cell Proliferation ,chemistry.chemical_classification ,Aniline Compounds ,biology ,Cell Cycle ,Aromatic amine ,Stereoisomerism ,Tubulin Modulators ,chemistry ,Cell culture ,Apoptosis ,Cancer cell ,biology.protein ,Molecular Medicine ,Drug Screening Assays, Antitumor ,Growth inhibition ,Aliphatic compound - Abstract
Compounds 2a- h and 6 displayed significant GI 50 values of 10(-7)-10(-6) M against various cancer cell lines. Of these compounds, 2-(6-(2-trifluoromethylphenyl))-3(Z)-hexen-1,5-diynyl)aniline (2c) showed the most potent growth inhibition activity. Compound 2c also arrested cancer cells in the G2/M phase and in low concentration reduced a significant percentage of MDA-MB-231/ATCC breast cancer tetraploid cells. In addition to the G2/M block, compound 2c caused microtubule depolymerization and induced apoptosis via activation of the caspase family.
- Published
- 2008
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