Novel N-hydroxybenzamide-based HDAC inhibitors with branched CAP group |
| |
Authors: | Hong Su Liqin Yu Angela Nebbioso Vincenzo Carafa Yadong Chen Lucia Altucci Qidong You |
| |
Affiliation: | aSchool of Pharmacy, China Pharmaceutical University, Nanjing 210009, China;bDipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico Luigi De Crecchio 7, 80138 Napoli, Italy |
| |
Abstract: | Ongoing effort to gather further knowledge about the structural requirements on histone deacetylase inhibitors led to the synthesis of novel N-hydroxybenzamide-based HDAC inhibitors 1a–o, introducing branched hydrophobic groups at the capping group, and their inhibition activity against HDACs and anti-proliferation activity in four tumor cell lines were determined. Compounds 1j–o were further tested against recombinant human HDAC1 and HDAC4 to evaluate their selectivity profile. This work further suggests that the chemical nature of the capping group is critical for subtle discrimination between the class I and the class II HDAC isoforms. |
| |
Keywords: | HDAC inhibitors N-Hydroxybenzamide Hydroxamic acid Selectivity Anti-tumor Anti-proliferation |
本文献已被 ScienceDirect 等数据库收录! |