title: Synthesis, anti-cancer evaluation of benzenesulfonamide derivatives as potent tubulin-targeting agents.
abstract: A series of benzenesulfonamide derivatives were synthesized and evaluated for their anti-proliferative activity and interaction with tubulin. These new derivatives showed significant activities against cellular proliferative and tubulin polymerization. Compound BA-3b proved to be the most potent compound with IC50 value ranging from 0.007 to 0.036 μM against seven cancer cell lines, and three drug-resistant cancer cell lines, which indicated a promising anti-cancer agent. The target tubulin was also verified by dynamic tubulin polymerization assay and tubulin intensity assay.
authors.affiliation: The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Jun
authors.initials: J
authors.lastname: Yang
authors.affiliation: The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Simin
authors.initials: S
authors.lastname: Yang
authors.affiliation: The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Shanshan
authors.initials: S
authors.lastname: Zhou
authors.affiliation: The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Dongbo
authors.initials: D
authors.lastname: Lu
authors.affiliation: The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Liyan
authors.initials: L
authors.lastname: Ji
authors.affiliation: The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Zhongjun
authors.initials: Z
authors.lastname: Li
authors.affiliation: The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: swang_yu@bjmu.edu.cn.
authors.forename: Siwang
authors.initials: S
authors.lastname: Yu
authors.affiliation: The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: xbmeng@bjmu.edu.cn.
authors.forename: Xiangbao
authors.initials: X
authors.lastname: Meng
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D062105:Molecular Docking Simulation; D055503:Protein Multimerization; D020836:Protein Structure, Quaternary; D012995:Solubility; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D014404:Tubulin / Q000737:chemistry* / Q000378:metabolism; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D014867:Water / Q000737:chemistry; D000096926:Benzenesulfonamides
chemical_list: D000970:Antineoplastic Agents; D013449:Sulfonamides; D014404:Tubulin; D050257:Tubulin Modulators; D014867:Water; D000096926:Benzenesulfonamides
keywords: Benzodiazepine; Benzothiazepine; Benzoxazepine; Sulfonamides; Tubulin-targeting agents