RIGID ANALOGS OF CAMPTOTHECIN AS DNA TOPOISOMERASE-I INHIBITORS
RIGID ANALOGS OF CAMPTOTHECIN AS DNA TOPOISOMERASE-I INHIBITORS
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DOI：
10.1021/jm00006a008
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发表时间：
1995-03-17
影响因子：
7.3
通讯作者：
STERNBACH, DD
中科院分区：
文献类型：
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作者：
LACKEY, K;BESTERMAN, JM;STERNBACH, DD
合成了取代的8-乙基-2-（2-氧代-1，2-二氢吲哚-3-亚基）-8-羟基-2，3，5，8-四氢-6-氧杂-3a-氮杂环戊二烯并[B]萘-1，4，7-三酮，并在体外可裂解复合物试验中评价了其作为拓扑异构酶I抑制剂的活性。这些化合物的活性可能归因于其刚性的平面几何形状，并试图将该系列中的SAR与喜树碱的已知属性相关联。
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.