Synthesis and biological evaluation of acylthiourea against DUSP1 inhibition

Bo Yeon Kim; Ji Hee Yoon; Myeongbin Kim; Jae Nyoung Kim; Hwangseo Park; Seong Eon Ryu; Sangku Lee

doi:10.1016/j.bmcl.2019.05.021

Synthesis and biological evaluation of acylthiourea against DUSP1 inhibition

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1746-1748. doi: 10.1016/j.bmcl.2019.05.021. Epub 2019 May 14.

Authors

Bo Yeon Kim¹, Ji Hee Yoon¹, Myeongbin Kim², Jae Nyoung Kim³, Hwangseo Park⁴, Seong Eon Ryu⁵, Sangku Lee⁶

Affiliations

¹ Anticancer Agent Research Center, KRIBB, Cheongju 28116, Republic of Korea.
² Department of Bioengineering, Hanyang University, Seoul 04763, Republic of Korea.
³ Department of Chemistry, Chonnam National University, Gwangju 61186, Republic of Korea.
⁴ Department of Bioscience and Biotechnology, Sejong University, Seoul 05006, Republic of Korea.
⁵ Department of Bioengineering, Hanyang University, Seoul 04763, Republic of Korea. Electronic address: ryuse@hanyang.ac.kr.
⁶ Anticancer Agent Research Center, KRIBB, Cheongju 28116, Republic of Korea. Electronic address: sangku@kribb.re.kr.

PMID: 31103445
DOI: 10.1016/j.bmcl.2019.05.021

Abstract

Structure based virtual screening attempts to discover DUSP1 inhibitors have yielded a scaffold featuring benzoxazole and acylthiourea pharmacophore. A series of its analogues were synthesized to explore structure activity relationship (SAR) of DUSP1 inhibition.

Keywords: Cancer; Dual specificity phosphatase; Enzyme inhibition; Mitogen-activated protein kinase; Structure activity relationship.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Dual Specificity Phosphatase 1 / antagonists & inhibitors*
Humans
Structure-Activity Relationship

Substances

DUSP1 protein, human
Dual Specificity Phosphatase 1