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ChemInform Abstract: 2-(2′-(Dimethylamino)ethyl)-1,2-dihydro-3H-dibenz(de,h)isoquinoline-1, 3-diones with Substituents at Positions 4, 8, 9, 10, and 11. Synthesis, Antitumor Activity, and Quantitative Structure-Activity Relationships.

✍ Scribed by S. M. SAMI; R. T. DORR; D. S. ALBERTS; A. M. SOLYOM; W. A. REMERS

Publisher: John Wiley and Sons
Year: 2010
Weight: 38 KB
Volume: 28
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199714122

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✦ Synopsis

2-(2'-(Dimethylamino)ethyl)-1,2-dihydro-3Hdibenz(de,h)isoquinoline-1, 3-diones with Substituents at Positions 4, 8, 9, 10, and 11. Synthesis, Antitumor Activity, and Quantitative Structure-Activity Relationships.

-Twenty-four new title compounds are synthesized following standard routes as described for (V) and (XIX). Anomalous reaction occurs with ( X) or (XIV) leading to unexpected (XI) and (XIII) or (XVI) besides the desired title compounds (XII) or (XV). Structureactivity relationship (SAR) studies reveal that lipophilicity increases DNA binding whereas large substituents decrease it and that DNA binding strength influences cytotoxic potency. Surprisingly, compound (VII), which binds very weakly to DNA, has substantial potency against leukemia cells. Synthesis and SAR studies of C-5 substituted title compounds are of interest. -(SAMI, S.

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