Anticancer activity of indolocarbazoles

作者：Chen Suting; You Qidong^*

来源：Progress in Chemistry, 2008, 20(2-3): 368-374.

• indolocarbazoles
• topoisomerases
• protein kinases
• DNA-Topo I complex
• cyclin-CDK complex
• structure-activity relationship (SAR)

Indolocarbazole is a kind of alkaloid extracted by microbe fermentation. These compounds, including their derivatives, such as staurosporine, ED-110, NB-506, rebeccamycin, azaindolocarbazole, indolocarbazole glycosides and bisindolylmaleimides, can act on many targets to exert anticancer function. It is now known that indolocarbazoles are effective topoisomerase poisons, and that they also inhibit protein kinases by competitively combining special amino acid groups of the ATP pocket, which later causes the cell arrest in the G1 phase. During the recent years, researchers endeavored to look for better forms of these chemicals to act as selective inhibitors with improved anticancer activity. This review will mainly discuss the research progress, clinical applications, anticancer activity mechanism, and the structure-activity relationship (SAR) of indolocarbazole derivatives.

• 出版日期2008-3
• 单位中国药科大学