Conformationally Locked Calixarene-Based Histone Deacetylase Inhibitors
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- 作者：Maria Giovanna Chini ; Stefania Terracciano ; Raffaele Riccio ; Giuseppe Bifulco ; Roberta Ciao ; Carmine Gaeta ; Francesco Troisi ; Placido Neri
- 刊名：Organic Letters
- 出版年：2010
- 出版时间：December 3, 2010
- 年：2010
- 卷：12
- 期：23
- 页码：5382-5385
- 全文大小：253K
- 年卷期：v.12,no.23(December 3, 2010)
- ISSN：1523-7052
文摘
Alkyl- and arylamidocalix[4]arene derivatives 1−11 have been designed and theoretically evaluated by docking studies as potential histone deacetylase inhibitors (HDACi). On the basis of the trimodal distribution of the calculated inhibition constants (Ki), five alkyl- or arylamido derivatives (3, 7, 8, 9, and 11) were synthesized and tested. A qualitative accordance between the experimental results and the theoretical predictions was obtained, confirming that appropriately substituted arylamidocalix[4]arenes are active HDACi.