2. Academic Validation
  3. Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer

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

  • Bioorg Med Chem. 2018 Feb 1;26(3):590-602. doi: 10.1016/j.bmc.2017.12.020.
Andrii Monastyrskyi 1,  Napon Nilchan 1,  Victor Quereda 2,  Yoshihiko Noguchi 1,  Claudia Ruiz 2,  Wayne Grant 2,  Michael Cameron 2,  Derek Duckett 2,  William Roush 3
Affiliations

Affiliations

  • 1 Department of Chemistry, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
  • 2 Department of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
  • 3 Department of Chemistry, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States. Electronic address: roush@scripps.edu.
PMID: 29289448 DOI: 10.1016/j.bmc.2017.12.020
Abstract

Casein Kinase 1δ/ε 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 CK1δ/ε 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.

Keywords

Breast cancer; Casein kinase 1 delta and epsilon; Inhibitor; Kinase; Structure-activity relationship.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z