Biomimetic semi-synthesis of fradcarbazole A and its analogues
Biomimetic semi-synthesis of fradcarbazole A and its analogues
复制标题
弗拉咔唑A及其类似物的仿生半合成
DOI：
10.1016/j.tet.2015.08.065
复制
发表时间：
2015-10-21
期刊：
影响因子：
2.1
通讯作者：
Zhu, Weiming
中科院分区：
文献类型：
--
作者：
Wang, Liping;Mei, Xiangui;Zhu, Weiming
利用仿生分子内环/脱水构造了星孢素-噻唑-吲哚骨架，首次合成了fradcarbazole A(1)。用同样的方法合成了苯类和恶唑类fradcarbazole A（2-4）。化合物1-4对A549细胞株的IC50值为0.4-3.6 μ M，在10 μ M时诱导G(0)/G(1)阻滞A549细胞周期，抑制pk - β激酶的IC50值为0.5-0.9 μ W. (C) 2015 Elsevier Ltd.。版权所有。
The first synthesis of fradcarbazole A (1) has been accomplished by using a biomimetic intramolecular cyclization/dehydration to construct the staurosporine-thiazole-indole skeleton. The phenyl and oxazole analogues of fradcarbazole A (2-4) were also synthesized using the same strategy. Compounds 1-4 displayed cytotoxicity against A549 cell line with IC50 values of 0.4-3.6 mu M, induction of G(0)/G(1) arrest of A549 cell cycle at 10 mu M, and inhibition of PK-beta kinase with IC50 values of 0.5-0.9 mu W. (C) 2015 Elsevier Ltd. All rights reserved.