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
Histone Deacetylase and Microtubules as Targets for the Synthesis of Releasable Conjugate Compounds / D. Passarella, D. Comi, A. Vanossi, G. Paganini, F. Colombo, L. Ferrante, V. Zuco, B. Danieli, F. Zunino. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 19:22(2009), pp. 6358-6363.
Histone Deacetylase and Microtubules as Targets for the Synthesis of Releasable Conjugate Compounds
D. PassarellaPrimo
;D. ComiSecondo
;L. Ferrante;B. DanieliPenultimo
;
2009
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 potencyFile | Dimensione | Formato | |
---|---|---|---|
manuscript-Passarella.doc
accesso aperto
Tipologia:
Post-print, accepted manuscript ecc. (versione accettata dall'editore)
Dimensione
1.12 MB
Formato
Microsoft Word
|
1.12 MB | Microsoft Word | Visualizza/Apri |
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.