Rigid analogs of camptothecin as DNA topoisomerase I inhibitors.
作者信息
Lackey K, Besterman J M, Fletcher W, Leitner P, Morton B, Sternbach D D
机构信息
Glaxo Research Institute, Research Triangle Park, North Carolina 27709.
出版信息
J Med Chem. 1995 Mar 17;38(6):906-11. doi: 10.1021/jm00006a008.
PMID:7699706
Abstract
Substituted 8-ethyl-2-(2-oxo-1,2-dihydroindol-3-ylidene)-8-hydroxy-2,3,5,8- tetrahydro-6-oxa-3a-azacyclopenta[b]naphthalene-1,4,7-triones were synthesized and evaluated as topoisomerase I inhibitors in an in vitro cleavable complex assay. The activity of these compounds may be attributed to their rigid, planar geometry, and an attempt was made to correlate the SAR in this series to known attributes of camptothecin.
摘要
Zotero 插件