STRUCTURE OF CURACIN-A, A NOVEL ANTIMITOTIC, ANTIPROLIFERATIVE, AND BRINE SHRIMP TOXIC NATURAL PRODUCT FROM THE MARINE CYANOBACTERIUM LYNGBYA-MAJUSCULA

被引:305
作者
GERWICK, WH
PROTEAU, PJ
NAGLE, DG
HAMEL, E
BLOKHIN, A
SLATE, DL
机构
[1] NCI,DIV CANC TREATMENT,DEV THERAPEUT PROGRAM,MOLEC PHARMACOL LAB,BETHESDA,MD 20892
[2] SYNTEX DISCOVERY RES CORP,INST BIOCHEM & CELL BIOL,PALO ALTO,CA 94304
关键词
D O I
10.1021/jo00085a006
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Bioassay-guided fractionation of the organic extract of a Curacao collection of Lyngbya majuscula led to the isolation of a new lipid, curacin A, with exceptional brine shrimp toxic and antiproliferative activities. Its unique thiazoline-containing structure has been deduced from spectroscopic information. Pure curacin A is an antimitotic agent (IC50 values in three cell lines ranging from 7 to 200 nM) that inhibits microtubule assembly and the binding of colchicine to tubulin.
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页码:1243 / 1245
页数:3
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