会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 60. 发明授权
    • Certain polycyclic compounds useful as tubulin-binding agents
    • 某些多环化合物可用作微管蛋白结合剂
    • US06433187B1
    • 2002-08-13
    • US09464217
    • 1999-12-15
    • David ClarkWalter FrankmoelleJonathan HouzeJuan C. JaenJulio C. Medina
    • David ClarkWalter FrankmoelleJonathan HouzeJuan C. JaenJulio C. Medina
    • C07D33708
    • C07D401/06A61K31/382C07C311/20C07C311/21C07C2603/30C07C2603/32C07D409/06C07D409/14C07D493/04
    • Derivatives of known tubulin-binding compounds are provided in which a (poly)fluorobenzene, a fluoropyridine, or a fluoronitrobenzene moiety is incorporated or added to the structure. These derivatives can be used as antimitotic agents and can be considered covalent modifiers of tubulin. The strategy developed for each of the compounds is to i) append a fluorinated electrophile (e.g., pentafluorophenylsulfonamido, 2-fluoropyridyl, or 3,5-dinitro-4-fluorophenyl) to an existing functional group in a natural product, ii) replace an aromatic ring in a natural product with a fluorinated electrophile, or iii) attach a fluorinated electrophile to an open valence in a portion of the molecule that will not interfere with recognition and binding to the tubulin site. Derivatives are provided based on colchicine, steganacin, podophyllotoxin, nocodazole, combretastatin, curacin A, vinblastine, vincristine, dolastatin, 2-methoxyestradiol, dihydroxy-pentamethoxyflavanone and others.
    • 提供了已知的微管蛋白结合化合物的衍生物,其中(聚)氟苯,氟代吡啶或氟硝基苯部分被结合或添加到该结构中。 这些衍生物可用作抗有丝分裂剂并且可以被认为是微管蛋白的共价修饰剂。 为每种化合物制定的策略是i)将天然产物中的现有官能团上的氟化亲电体(例如五氟苯基磺酰胺基,2-氟吡啶基或3,5-二硝基-4-氟苯基) 具有氟化亲电体的天然产物中的芳香环,或iii)在分子的一部分中将氟化亲电体连接至开放价态,其不会干扰识别和结合微管蛋白位点。 衍生物基于秋水仙碱,steganacin,鬼臼毒素,诺考达唑,考布他汀,curacin A,长春花碱,长春新碱,多卡他汀,2-甲氧基雌二醇,二羟基 - 五甲氧基黄酮等。