Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors
| Autor: | Pengyu Qian, Ming Xu, Ning Xie, Yongzhen Wang, Yanyang Li, Yanjin Zhao, Shuxin Li |
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| Rok vydání: | 2014 |
| Předmět: |
Stereochemistry
Biological Availability Antineoplastic Agents Histone Deacetylases Rats Sprague-Dawley chemistry.chemical_compound Structure-Activity Relationship Drug Discovery Tumor Cells Cultured Moiety Animals Humans Cell Proliferation Pharmacology Bicyclic molecule Dose-Response Relationship Drug Molecular Structure Organic Chemistry General Medicine HCT116 Cells Combinatorial chemistry Rats Histone Deacetylase Inhibitors chemistry Design synthesis Cell culture Drug Design Benzamides MCF-7 Cells Female Drug Screening Assays Antitumor Lead compound Human cancer |
| Zdroj: | European journal of medicinal chemistry. 100 |
| ISSN: | 1768-3254 |
| Popis: | Guided by the principle of nonclassical electronic isosterism and structural optimization, a series of novel HDAC inhibitors bearing a bicyclic heterocycle moiety were designed and synthesized based on the lead compound of MS-275. All the prepared compounds were evaluated for their in vitro antiproliferative activities against HCT-116, MCF-7 and A549 human cancer cell lines, all compounds exerted excellent antitumor activities. Moreover, the compound 4a exhibited an acceptable pharmacokinetic profile with bio-availability in rat of 76% and could be considered as a candidate compound for further development. |
| Databáze: | OpenAIRE |
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