The Effect of Vicinal Difluorination on the Conformation and Potency of Histone Deacetylase Inhibitors

被引：5

作者：

Ariawan, A. Daryl ^{[1
]}

Mansour, Flora ^{[1
]}

Richardson, Nicole ^{[1
]}

Bhadbhade, Mohan ^{[2
]}

Ho, Junming ^{[1
]}

Hunter, Luke ^{[1
]}

机构：

[1] UNSW Sydney, Sch Chem, Sydney, NSW 2052, Australia

[2] UNSW Sydney, Mark Wainwright Analyt Ctr, Sydney, NSW 2052, Australia

来源：

MOLECULES | 2021年 / 26卷 / 13期

关键词：

SAHA; Scriptaid; stereoselective fluorination; HDAC; FLUORINATION; CYCLIZATION;

D O I：

10.3390/molecules26133974

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Histone deacetylase enzymes (HDACs) are potential targets for the treatment of cancer and other diseases, but it is challenging to design isoform-selective agents. In this work, we created new analogs of two established but non-selective HDAC inhibitors. We decorated the central linker chains of the molecules with specifically positioned fluorine atoms in order to control the molecular conformations. The fluorinated analogs were screened against a panel of 11 HDAC isoforms, and minor differences in isoform selectivity patterns were observed.

引用

页数：17

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