On topography and functionality in the B-D rings of cephalostatin cytotoxins

被引：21
作者：
LaCour, TG [1 ]
Guo, CX
Ma, SH
Jeong, JU
Boyd, MR
Matsunaga, S
Fusetani, N
Fuchs, PL
机构：
[1] Purdue Univ, Dept Chem, W Lafayette, IN 47907 USA
[2] NCI, Frederick Canc Res & Dev Ctr, Frederick, MD 21702 USA
[3] Univ Tokyo, Marine Biochem Lab, Bunkyo Ku, Tokyo 113, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 17期
关键词：
D O I：
10.1016/S0960-894X(99)00430-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Analogues 12'beta-hydroxycephalostatin 1 (9), 7'-deoxyritterazine G (10), and 14-epi-7'-deoxyritterazine B (11) were prepared via our protocol for unsymmetrical pyrazine synthesis. Cytotoxicity against human tumors was also determined for the first time for ritterazines, with femtomolar potency and a high correlation to cephalostatins observed. The SAR of these and related. compounds provide insight into the importance of topography and certain chemical functionality in the B-D and B'-D' rings of cephalostatin type antineoplastics. (C) 1999 Elsevier Science Ltd. All rights reserved.
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页码：2587 / 2592
页数：6
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