On the relationship of OSW-1 to the cephalostatins

On the relationship of OSW-1 to the cephalostatins
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DOI:
10.1016/s0960-894x(98)00743-4
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发表时间:
1999-02-08
影响因子:
2.7
通讯作者:
Fuchs, PL
Fuchs, PL
中科院分区:
医学4区
文献类型:
--
作者:
Guo, CX;LaCour, TG;Fuchs, PL

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皂苷 OSW-1 的抗肿瘤双甾体(头孢他汀型)类似物是由 OSW-1 的二氢苷元生产的。关键糖苷配基 6H 是通过 8 个步骤从 5 α-androstan-3 beta-ol-17-one 获得的(产率 38%)。糖苷配基、中间体和混合类似物的 SAR 提供了有关 C22-氧碳鎓离子在 OSW-1 和头孢他汀生物活性中的共同作用的见解 (C) 1999 Elsevier Science Ltd。保留所有权利。
Antineoplastic bis-steroidal (cephalostatin-type) analogues of the saponin OSW-1 were produced from a dihydroaglycone of OSW-1. The key aglycone 6H was obtained from 5 alpha-androstan-3 beta-ol-17-one in 8 steps (38% yield). The SAR of the aglycones, intermediates, and hybrid analogues provide insights regarding the proposed common role of C22-oxocarbenium ions in the bioactivity of both OSW-1 and cephalostatins (C) 1999 Elsevier Science Ltd. All rights reserved.