title: 2-(6-aryl-3(Z)-hexen-1,5-diynyl)anilines as a new class of potent antitubulin agents.
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.
authors.affiliation: Graduate Institute of Pharmaceutical Sciences, Graduate Institute of Biochemistry, Kaohsiung Medical University, Kaohsiung, Taiwan.
authors.forename: Yu-Hsiang
authors.initials: YH
authors.lastname: Lo
authors.forename: Ching-Chih
authors.initials: CC
authors.lastname: Lin
authors.forename: Chi-Fong
authors.initials: CF
authors.lastname: Lin
authors.forename: Ying-Ting
authors.initials: YT
authors.lastname: Lin
authors.forename: Tsai-Hui
authors.initials: TH
authors.lastname: Duh
authors.forename: Yi-Ren
authors.initials: YR
authors.lastname: Hong
authors.forename: Sheng-Huei
authors.initials: SH
authors.lastname: Yang
authors.forename: Shinne-Ren
authors.initials: SR
authors.lastname: Lin
authors.forename: Shyh-Chyun
authors.initials: SC
authors.lastname: Yang
authors.forename: Long-Sen
authors.initials: LS
authors.lastname: Chang
authors.forename: Ming-Jung
authors.initials: MJ
authors.lastname: Wu
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001704:Biopolymers; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008870:Microtubules / Q000187:drug effects / Q000648:ultrastructure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000737:chemistry; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: C529815:2-(6-(2-trifluoromethylphenyl))-3-(hexen-1,5-diynyl)aniline; D000814:Aniline Compounds; D001704:Biopolymers; D014404:Tubulin; D050257:Tubulin Modulators