Synthesis and biological activities of reveromycin A and spirofungin A derivatives

Synthesis and biological activities of reveromycin A and spirofungin A derivatives
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DOI:
10.1016/j.bmcl.2008.05.054
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发表时间:
2008-07-01
影响因子:
2.7
通讯作者:
Sodeoka, Mikiko
Sodeoka, Mikiko
中科院分区:
医学4区
文献类型:
--
作者:
Shimizu, Takeshi;Usui, Takeo;Sodeoka, Mikiko

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合成了真核细胞生长抑制剂回复霉素A(reveromycin A)和螺芬菌素A(spirofungin A)的各种衍生物,重点研究了它们对异亮氨酰-tRNA合成酶活性和破骨细胞存活的抑制作用,以及对src(ts)-NRK细胞形态逆转的抑制作用。结果表明,2,3-二氢回复霉素A是一种很有前途的回复霉素A衍生物。(C)2008爱思唯尔有限公司保留所有权利。
Various derivatives of reveromycin A, an inhibitor of eukaryotic cell growth, and spirofungin A, focusing on the 5S hydroxyl group and C18 hemisuccinyl group, were synthesized and their inhibitory effects on both the isoleucyl-tRNA synthetase activity and the survival of osteoclasts, and activities on the morphological reversion of src(ts)-NRK cells were examined. It was found that 2,3-dihydroreveromycin A is the promising derivative of reveromycin A based on the activity and stability. (C) 2008 Elsevier Ltd. All rights reserved.