C10-substituted camptothecin analogs
    2.
    发明授权
    C10-substituted camptothecin analogs 有权
    C10取代的喜树碱类似物

    公开(公告)号:US07687497B2

    公开(公告)日:2010-03-30

    申请号:US11974756

    申请日:2007-10-16

    摘要: The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW

    摘要翻译: 本发明的新颖的C10修饰的喜树碱类似物及其药学上可接受的盐:(i)具有有效的抗肿瘤活性(即纳米摩尔或亚纳摩尔浓度),用于在体外抑制人和动物肿瘤细胞的生长; (ii)是拓扑异构酶I的有效抑制; (iii)对MDR / MRP耐药性不敏感; (iv)不需要代谢药物活化:(v)缺乏A环或B环的葡糖醛酸化; (vi)降低与血浆蛋白质的药物结合亲和力; (vii)维持内酯稳定性; (viii)维持药物效力; 和(ix)具有低分子量(例如MW <600)。