Publications by Hanyue Zhong

Publications by authors named "Hanyue Zhong"

Page 1 of 1

Discovery of ()--(2-Amino-4-fluorophenyl)-4-(1-(3-(4-((dimethylamino)methyl)phenyl)-6-oxopyridazin-1(6)-yl)ethyl)benzamide as Potent Class I Selective HDAC Inhibitor for Oral Anticancer Drug Candidate.

Daqiang Li Zhuo Zhang Yalei Li Xinyi Wang Hanyue Zhong

J Med Chem

May 2023

Article Synopsis

A new series of benzamide derivatives were created from a pyridazinone scaffold, with one specific compound showing strong inhibition of human HDAC isoforms and effective anti-cancer activity against SKM-1 cancer cells.
This compound increased acetyl-histone H3 and P21 levels, inducing G1 cell cycle arrest and apoptosis, which led to successful oral antitumor effects in innovative xenograft models.
The compound demonstrated favorable pharmacokinetics and minimal adverse effects on the heart’s hERG channel, suggesting its potential as a new drug candidate for further research.

View Article and Find Full Text PDF

Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold.

Jingjing Chen Huixin He Aihuan Wei Yalei Li Gang Cheng Hanyue Zhong

Eur J Med Chem

June 2022

Novel pyrrolopyridone BET degraders were designed and synthesized based on the binding mode between the pyrrolopyridone BET inhibitor with the BRD4 protein. The potent degraders on MV-4-11 cells were discovered through structure-activity relationship study. Modification of warhead on pyrrolopyridone BET degraders significantly regulates BRD4 isoform (long and short) protein degradation, which induces differential cell cycle arrest and apoptosis on MV-4-11 cells.

View Article and Find Full Text PDF