Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer

被引：24

作者：

Monastyrskyi, Andrii ^{[1
]}

Nilchan, Napon ^{[1
]}

Quereda, Victor ^{[2
]}

Noguchi, Yoshihiko ^{[1
]}

Ruiz, Claudia ^{[2
]}

Grant, Wayne ^{[2
]}

Cameron, Michael ^{[2
]}

Duckett, Derek ^{[2
]}

Roush, William ^{[1
]}

机构：

[1] Scripps Florida, Dept Chem, 130 Scripps Way, Jupiter, FL 33458 USA

[2] Scripps Florida, Dept Mol Med, 130 Scripps Way, Jupiter, FL 33458 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2018年 / 26卷 / 03期

关键词：

Casein kinase 1 delta and epsilon; Kinase; Inhibitor; Structure-activity relationship; Breast cancer; CYCLIN-DEPENDENT KINASES; ONE-POT SYNTHESIS; SELECTIVE-INHIBITION; CIRCADIAN-RHYTHMS; ACCURATE DOCKING; IN-VITRO; PROTEIN; EPSILON; PHOSPHORYLATION; FAMILY;

D O I：

10.1016/j.bmc.2017.12.020

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：

Casein kinase 1 delta/epsilon have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1 delta/epsilon inhibitors 17 and 28 displaying low nanomolar values in antiproliferative assays against the human MDA-MB-231 triple negative breast cancer cell line and have physical, in vitro and in vivo pharmacokinetic properties suitable for use in proof of principle animal xenograft studies against human cancers. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：590 / 602

页数：13

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