期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 14, 期 4, 页码 901-904出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2003.12.017
关键词
DNA binding; pyrrolobenzodiazepines; PBDs; sequence-selective; gene targeting
We report examples of a series of novel pyrrolo[2,1-c][1,4]benzodiazepine (PBD) analogues 12-15 prepared from a common functionalized building block 11 that can be conveniently synthesized on a large scale and in optically pure form. Isoindoline analogue 15 is the most cytotoxic agent in this series, has the highest DNA-binding affinity, and shows significant activity in the in vivo hollow fibre assay. (C) 2004 Elsevier Ltd. All rights reserved.
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