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2-(6-Aryl-3(Z)-hexen-1,5-diynyl)anilines as a New Class of Potent Antitubulin Agents
- Source :
- Journal of Medicinal Chemistry. 51:2682-2688
- Publication Year :
- 2008
- Publisher :
- American Chemical Society (ACS), 2008.
-
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.
- 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
Subjects
Details
- ISSN :
- 15204804 and 00222623
- Volume :
- 51
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....132878e54c37a707df59ba3d59761e02