Title of article
Synthesis and biological evaluation of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) C8 cyclic amine conjugates
Author/Authors
Luke A. Masterson، نويسنده , , Stephen J. Croker، نويسنده , , Terence C. Jenkins، نويسنده , , Philip W. Howard، نويسنده , , David E. Thurston، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
901
To page
904
Abstract
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.
Keywords
DNA binding , Pyrrolobenzodiazepines , Sequenceselective , Gene targeting. , PBDs
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794098
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