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Synthesis and biological evaluation of pyrimidine derivatives as novel human Pin1 inhibitors.

Abstract：

:Pin1 (Protein interacting with NIMA1) is a cis-trans isomerase and promotes the amide bond rotation of phosphoSer/Thr-Pro motifs in its substrates. Inhibition of Pin1 might be a novel strategy for developing anticancer agents. Herein, a series of pyrimidine derivatives were synthesized and their Pin1 inhibitory activities were evaluated. Among them, four compounds (2a, 2f, 2h and 2l) displayed potent inhibitory activities against Pin1 with IC50 values lower than 3 µM. This series of pyrimidine-based inhibitors presented time-dependent inhibition against Pin1. The structure-activity relationships on the 2-, 4- and 5-positions of the pyrimidine ring were analyzed in details, which would facilitate further exploration of new Pin1 inhibitors.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Cui G,Jin J,Chen H,Cao R,Chen X,Xu B

doi

10.1016/j.bmc.2018.03.024

subject

Has Abstract

pub_date

2018-05-01 00:00:00

pages

2186-2197

issue

8

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(18)30258-X

journal_volume

26

pub_type

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