title: N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling.
abstract: A series of N-sulfonyl-aminobiaryl derivatives have been examined as novel antitubulin agents. Compound 21 [N-(4'-cyano-3'-fluoro-biphenyl-2-yl)-4-methoxy-benzenesulfonamide] exhibits remarkable antiproliferative activity against four cancer cell lines (pancreatic AsPC-1, lung A549, liver Hep3B, and prostate PC-3) with a mean GI50 value of 57.5 nM. Additional assays reveal that 21 inhibits not only tubulin polymerization but also the phosphorylation of STAT3 inhibition with an IC50 value of 0.2 μM. Four additional compounds (8, 10, 19, and 35) are also able to inhibit this phosphorylation. This study describes novel N-sulfonyl-aminobiaryl (biaryl-benzenesulfonamides) as potent anticancer agents targeting both STAT3 and tubulin.
authors.affiliation: Translational Research Center, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.
authors.forename: Mei-Jung
authors.initials: MJ
authors.lastname: Lai
authors.affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.
authors.forename: Hsueh-Yun
authors.initials: HY
authors.lastname: Lee
authors.affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.
authors.forename: Hsun-Yueh
authors.initials: HY
authors.lastname: Chuang
authors.affiliation: School of Pharmacy, College of Medicine, National Taiwan University , Taipei, Taiwan.
authors.forename: Li-Hsun
authors.initials: LH
authors.lastname: Chang
authors.affiliation: The Ph.D program for Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.
authors.forename: An-Chi
authors.initials: AC
authors.lastname: Tsai
authors.affiliation: Ph.D. Program for the Clinical Drug Discovery from Botanical Herbs, College of Pharmacy, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.
authors.forename: Mei-Chuan
authors.initials: MC
authors.lastname: Chen
authors.affiliation: The Ph.D program for Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.
authors.forename: Han-Lin
authors.initials: HL
authors.lastname: Huang
authors.affiliation: Department of Pharmacology, College of Medicine, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.
authors.forename: Yi-Wen
authors.initials: YW
authors.lastname: Wu
authors.affiliation: School of Pharmacy, College of Medicine, National Taiwan University , Taipei, Taiwan.
authors.forename: Che-Ming
authors.initials: CM
authors.lastname: Teng
authors.affiliation: The Ph.D program for Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.|Department of Pharmacology, College of Medicine, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.
authors.forename: Shiow-Lin
authors.initials: SL
authors.lastname: Pan
authors.affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.
authors.forename: Yi-Min
authors.initials: YM
authors.lastname: Liu
authors.affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.
authors.forename: Samir
authors.initials: S
authors.lastname: Mehndiratta
authors.affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University , 250 Wuxing Street, Taipei 11031, Taiwan.|School of Pharmacy, National Defense Medical Center , Taipei, Taiwan.
authors.forename: Jing-Ping
authors.initials: JP
authors.lastname: Liou
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001667:Binding, Competitive / Q000187:drug effects; D045744:Cell Line, Tumor; D003078:Colchicine / Q000378:metabolism; D006801:Humans; D010766:Phosphorylation / Q000187:drug effects; D050796:STAT3 Transcription Factor / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D050796:STAT3 Transcription Factor; C494086:STAT3 protein, human; D013449:Sulfonamides; D050257:Tubulin Modulators; D003078:Colchicine