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.
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Authors | Juan Feng, Jian-Qi Li |
Journal | Yao xue xue bao = Acta pharmaceutica Sinica
(Yao Xue Xue Bao)
Vol. 44
Issue 12
Pg. 1376-82
(Dec 2009)
ISSN: 0513-4870 [Print] China |
PMID | 21351472
(Publication Type: English Abstract, Journal Article, Research Support, U.S. Gov't, Non-P.H.S.)
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Chemical References |
- Antineoplastic Agents
- Benzamides
- Histone Deacetylase Inhibitors
- benzamide
- Histone Deacetylases
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Topics |
- Antineoplastic Agents
(chemical synthesis, chemistry, pharmacology)
- Benzamides
(chemical synthesis, chemistry, pharmacology)
- Cell Line, Tumor
- Drug Screening Assays, Antitumor
- Histone Deacetylase Inhibitors
(chemical synthesis, chemistry, pharmacology)
- Histone Deacetylases
(metabolism)
- Humans
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