Synthesis and Anticancer Activity of New Hydroxamic Acid Containing 1,4-Benzodiazepines
- 11 March 2009
- journal article
- letter
- Published by American Chemical Society (ACS) in Organic Letters
- Vol. 11 (7), 1575-1578
- https://doi.org/10.1021/ol900210h
Abstract
By employing an intramolecular Pd(0)-mediated ring opening of an acylnitroso-derived cycloadduct, new hydroxamic acid containing benzodiazepines have been synthesized and have demonstrated biological activity in MCF-7 and PC-3 tumor cell lines. Subsequent N−O bond reduction of the hydroxamate has provided access to amide analogues for SAR studies. During the course of our syntheses, an intermediate oxazoline N-oxide was isolated and gave insight into the mechanism of the key Pd(0)-mediated reaction.Keywords
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