N-(氨基吡啶)苯甲酰胺衍生物的合成与抗肿瘤活性
[Synthesis and anti-tumor activities of N-(aminopyridine) benzamide derivaties].
作者信息
Feng Juan, Li Jian-Qi
机构信息
State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
出版信息
Yao Xue Xue Bao. 2009 Dec;44(12):1376-82.
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.
为了探索具有抗肿瘤活性的新型组蛋白去乙酰化酶（HDAC）抑制剂，在初步研究的基础上，设计并制备了16种N-(2-氨基-4-吡啶)苯甲酰胺衍生物（A类）和16种N-(2-氨基-3-吡啶)苯甲酰胺衍生物（B类），并分别通过1H NMR和HR-MS对其结构进行了确证。结果表明，除V-20和V-21外，30种目标化合物具有HDAC抑制活性，其中V-13、V-14、V-16在体外200 μmol·L-1时与CI-994活性相当。化合物V-30、V-31和V-32对Hut78、Jurkat E6-1、A549、K562和MDA-MB-435s表现出较强的抑制活性。
Zotero 插件