FENG Juan, LI Jian-Ji. Synthesis and anti-tumor activities of N-(aminopyridine) benzamide derivatiesJ. 药学学报, 2009,44(12): 1376-1382.
Citation: FENG Juan, LI Jian-Ji. Synthesis and anti-tumor activities of N-(aminopyridine) benzamide derivatiesJ. 药学学报, 2009,44(12): 1376-1382.

Synthesis and anti-tumor activities of N-(aminopyridine) benzamide derivaties

  • 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 -20 and -21 had HDACs inhibitory activity and -13, -14, -16 were equal to CI-994 at 200 μmol·L1 in vitro.  Compounds -30-31 and -32 exhibited potent inhibitory activities on Hut78Jurkat E6-1A549K562 and MDA-MB-435s.

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