Highly fluorescent and HDAC6 selective scriptaid analogues

被引：20

作者：

Fleming, Cassandra L. ^{[1
]}

Natoli, Anthony ^{[2
]}

Schreuders, Jeannette ^{[2
]}

Devlin, Mark ^{[2
]}

Yoganantharajah, Prusothman ^{[3
]}

Gibert, Yann ^{[3
]}

Leslie, Kathryn G. ^{[4
]}

New, Elizabeth J. ^{[4
]}

Ashton, Trent D. ^{[1
,5
,6
]}

Pfeffer, Frederick M. ^{[1
]}

机构：

[1] Deakin Univ, Sch Life & Environm Sci, Waurn Ponds, Vic 3216, Australia

[2] Peter MacCallum Canc Ctr, Melbourne, Vic 3000, Australia

[3] Deakin Univ, Sch Med, Waurn Ponds, Vic 3216, Australia

[4] Univ Sydney, Sch Chem, Sydney, NSW 2006, Australia

[5] Walter & Eliza Hall Inst Med Res, Parkville, Vic 3052, Australia

[6] Univ Melbourne, Dept Med Biol, Parkville, Vic 3010, Australia

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2019年 / 162卷

关键词：

Naphthalimide; Fluorescence; Imaging; Zebrafish; Scriptaid; 4MS; HDAC; HISTONE DEACETYLASE INHIBITOR; RUTHENIUM(II) POLYPYRIDYL COMPLEXES; IN-VITRO; CANCER; PROBE; COMBINATION; DISCOVERY; IDENTIFICATION; DISRUPTION; BORTEZOMIB;

D O I：

10.1016/j.ejmech.2018.11.020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Fluorescent scriptaid analogues with excellent HDAC6 selectivity (HDAC1/6 > 500) and potency (HDAC6 IC50 < 5 nM) have been synthesised and evaluated. The highly fluorescent nature of the compounds (up to Phi(F)= 0.83 in DMSO and 038 in aqueous buffer) makes them ideally suited for cellular imaging and visualisation of their cytoplasmic localisation was readily accomplished. Whole organism imaging in zebrafish confirmed both the vascular localisation of the new inhibitors and the impact of HDAC6 inhibition on in vivo development. Crown Copyright (C) 2018 Published by Elsevier Masson SAS. All rights reserved,

引用

页码：321 / 333

页数：13

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