title: [Synthesis and anti-tumor activities of N-(aminopyridine) benzamide derivaties].
abstract: To explore novel histone deacetylase (HDAC) inhibitors with anti-tumor activity, on the basis of preliminary studies, sixteen N-(2-amino-4-pyridine) benzamide derivaties (class A) and sixteen N-(2-amino-3-pyridine) benzamide derivaties (class B) were designed and prepared, and their structures were confirmed by 1H NMR and HR-MS individually. The results showed that 30 target compounds except V-20 and V-21 had HDACs inhibitory activity and V -13, V -14, V -16 were equal to CI-994 at 200 micromol x L(-1) in vitro. Compounds V-30, V-31 and V-32 exhibited potent inhibitory activities on Hut78, Jurkat E6-1, A549, K562 and MDA-MB-435s.
authors.affiliation: State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
authors.forename: Juan
authors.initials: J
authors.lastname: Feng
authors.forename: Jian-Qi
authors.initials: JQ
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006655:Histone Deacetylases / Q000378:metabolism; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D001549:Benzamides; D056572:Histone Deacetylase Inhibitors; C037689:benzamide; D006655:Histone Deacetylases