Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence |
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| Authors: | Hanessian Stephen Auzzas Luciana Giannini Giuseppe Marzi Mauro Cabri Walter Barbarino Marcella Vesci Loredana Pisano Claudio |
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| Institution: | Department of Chemistry, Université de Montréal, Station Centre-ville, Montréal, Quebec, Canada. stephen.hanessian@umontreal.ca |
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| Abstract: | A series of omega-alkoxy ethers were prepared with variation of the length of the aliphatic chain of suberoylanilide hydroxamic acid (SAHA, vorinostat). Eight carbon long chain analogues showed the best activity, among which several substituted benzyl ether derivatives exhibited inhibitory activity on HDAC comparable to SAHA, and antiproliferative activity on three human cell lines (NB4, H460, and HCT-116) better than SAHA. However, no significant difference in antiproliferative activity was observed between two enantiomers bearing the benzyl ether moiety. |
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