Strategies for the synthesis of N-(azacycloalkyl)bisindolylmaleimides:: selective inhibitors of PKCβ

被引:22
作者
Faul, MM [1 ]
Grutsch, JL [1 ]
Kobierski, ME [1 ]
Kopach, ME [1 ]
Krumrich, CA [1 ]
Staszak, MA [1 ]
Udodong, U [1 ]
Vicenzi, JT [1 ]
Sullivan, KA [1 ]
机构
[1] Eli Lilly & Co, Lilly Corp Ctr, Global Chem Proc Res & Dev, Indianapolis, IN 46285 USA
关键词
N-(azacycloalkyl)bisindolylmaleimides; angiogenesis; vascular endothelial growth factor;
D O I
10.1016/S0040-4020(03)00973-6
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
N-(Azacycloalkyl)bisindolylmaleimides 1 have been identified to be selective inhibitors of PKCbeta. This manuscript will describe the synthetic approaches employed to prepare this class of compounds that resulted in development of efficient methods for preparation of N-(azacycloalkyl) indole 5, indole-3-acetamide 8 and indole-3-glyoxylate ester 4 derivatives. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:7215 / 7229
页数:15
相关论文
共 24 条
[21]   AMINOHALOBORANE IN ORGANIC-SYNTHESIS .1. SPECIFIC ORTHO SUBSTITUTION-REACTION OF ANILINES [J].
SUGASAWA, T ;
TOYODA, T ;
ADACHI, M ;
SASAKURA, K .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1978, 100 (15) :4842-4852
[22]  
Thomas C, 1998, SYNTHESIS-STUTTGART, P1491
[23]   Characterization of vascular endothelial growth factor's effect on the activation of protein kinase C, its isoforms, and endothelial cell growth [J].
Xia, P ;
Aiello, LP ;
Ishii, H ;
Jiang, ZY ;
Park, DJ ;
Robinson, GS ;
Takagi, H ;
Newsome, WP ;
Jirousek, MR ;
King, GL .
JOURNAL OF CLINICAL INVESTIGATION, 1996, 98 (09) :2018-2026
[24]  
ZHANG JL, 1996, HUAXUE XUEBAO, P84