Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372718 | Bioorganic & Medicinal Chemistry Letters | 2009 | 6 Pages |
Abstract
Design and synthesis of an HDAC inhibitor and its merger with three tubulin binders to create releasable conjugate compounds is described. The biological evaluation includes: (a) in vitro reactivity with glutathione, (b) antiproliferative activity, (c) cell cycle analysis and (d) quantification of protein acetylation. The cellular pharmacology study indicated that the HDAC-inhibitor-drug conjugates retained antimitotic and proapoptotic activity with a reduced potency.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Daniele Passarella, Daniela Comi, Andrea Vanossi, Gianfranco Paganini, Francesco Colombo, Luca Ferrante, Valentina Zuco, Bruno Danieli, Franco Zunino,