6533b86ffe1ef96bd12ce8b6
RESEARCH PRODUCT
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
Marinella RobertiElisa GiacominiAlfonso CiottaAngela NebbiosoMaurizio RecanatiniFederico FalchiMaria Rosaria PipitoneAntonietta Di CristinaStefania GrimaudoLucia AltucciCristina IanniManlio Tolomeosubject
Multifunctional ligandsCell cycle progressionHDAC inhibitionInhibitory postsynaptic potentialBiochemistrySettore BIO/13 - Biologia ApplicataHDACDrug DiscoverymedicineCytotoxic T cellHDAC inhibition; Multifunctional ligands; antiproliferative activity; chimeric compound; stilbeneCancerbiologyChemistryANTIPROLIFERATIVE ACTIVITYOrganic ChemistryMultifunctional ligandsCancermultifunctional ligandmedicine.diseaseCombinatorial chemistrySettore CHIM/08 - Chimica FarmaceuticastilbeneHistoneBiochemistrySTILBENESbiology.proteinchimeric compoundHDAC INHIBITORSEpigeneticsHistone deacetylaseChimeric moleculesdescription
Given our interest in finding potential antitumor agents and in view of the multifactorial mechanistic nature of cancer, in the present work, taking advantage of the multifunctional ligands approach, new chimeric molecules were designed and synthesized by combining in single chemical entities structural features of SAHA, targeting histone deacetylases (HDACs), with substituted stilbene or terphenyl derivatives previously obtained by us and endowed with antiproliferative and pro-apoptotic activity. The new chimeric derivatives were characterized with respect to their cytotoxic activity and their effects on cell cycle progression on different tumor cell lines, as well as their HDACs inhibition. Among the other, trans -6 showed the most interesting biological profile, as it exhibited a strong pro-apoptotic activity in tumor cell lines in comparison with both of its parent compounds and a marked HDAC inhibition.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2014-07-08 |