1201937-87-2Relevant articles and documents
Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds
Passarella, Daniele,Comi, Daniela,Vanossi, Andrea,Paganini, Gianfranco,Colombo, Francesco,Ferrante, Luca,Zuco, Valentina,Danieli, Bruno,Zunino, Franco
supporting information; experimental part, p. 6358 - 6363 (2010/05/02)
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.
