Conformationally Locked Calixarene-Based Histone Deacetylase Inhibitors

[摘要]：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 (K-i), 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.

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