A review of progress in o-aminobenzamide-based HDAC inhibitors with dual targeting capabilities for cancer therapy

WX Zhang, J Huang, XY Tian, YH Liu, MQ Jia… - European journal of …, 2023 - Elsevier
Histone deacetylases, as a new class of anticancer targets, could maintain homeostasis by
catalyzing histone deacetylation and play important roles in regulating the expression of …

New drug approvals for 2022: Synthesis and clinical applications

S Yuan, DD Shen, R Jia, JS Sun… - Medicinal Research …, 2023 - Wiley Online Library
Abstract The US Food and Drug Administration has approved a total of 37 new drugs in
2022, which are composed of 20 chemical entities and 17 biologics. In particular, 20 …

DFRscore: deep learning-based scoring of synthetic complexity with drug-focused retrosynthetic analysis for high-throughput virtual screening

H Kim, K Lee, C Kim, J Lim, WY Kim - Journal of Chemical …, 2023 - ACS Publications
Recently emerging generative AI models enable us to produce a vast number of compounds
for potential applications. While they can provide novel molecular structures, the synthetic …

Annual review of PROTAC degraders as anticancer agents in 2022

X Wang, ZL Qin, N Li, MQ Jia, QG Liu, YR Bai… - European Journal of …, 2024 - Elsevier
Following nearly two decades of development, significant advancements have been
achieved in PROTAC technology. As of the end of 2022, more than 20 drugs have entered …

Tubulin degradation: Principles, agents, and applications

YF Zhang, J Huang, WX Zhang, YH Liu, X Wang… - Bioorganic …, 2023 - Elsevier
The microtubule system plays an important role in the mitosis and growth of eukaryotic cells,
and it is considered as an appealing and highly successful molecular target for cancer …

Is it still worth renewing nucleoside anticancer drugs nowadays?

ZQ Liu - European Journal of Medicinal Chemistry, 2023 - Elsevier
Highlights•Metabolic procedures of a nucleoside anticancer drug are summarized.•
Anticancer properties of newly synthesized nucleoside analogs are introduced.•Synthetic …

Discovery of novel arylamide derivatives containing piperazine moiety as inhibitors of tubulin polymerisation with potent liver cancer inhibitory activity

XY Shi, H Jiao, JK Zhang, XY Tian, DF Guo… - Journal of Enzyme …, 2023 - Taylor & Francis
In this work, a series of novel arylamide derivatives containing piperazine moiety were
designed and synthesised as tubulin polymerisation inhibitors. Among 25 target …

N-Benzyl arylamide derivatives as novel and potent tubulin polymerization inhibitors against gastric cancers: Design, structure–activity relationships and biological …

J Song, S Wang, Q Liu, X Wang, S Yuan, H Liu… - Chinese Chemical …, 2024 - Elsevier
In this work, we employed a ring-opening strategy to develop a series of novel N-benzyl
arylamide derivatives as tubulin polymerization inhibitors. Notably, 13n (MY-1388) exhibited …

Discovery of novel coumarin-based derivatives as inhibitors of tubulin polymerization targeting the colchicine binding site with potent anti-gastric cancer activities

XY Tian, WX Zhang, XY Chen, MQ Jia… - European Journal of …, 2024 - Elsevier
In this work, a series of novel coumarin-based derivatives were designed and synthesized
as tubulin polymerization inhibitors targeting the colchicine binding site, and their …

Design, synthesis and biological evaluation of novel 2, 4-diaminopyrimidine cinnamyl derivatives as inhibitors of FAK with potent anti-gastric cancer activities

Y Liu, LJ Kong, N Li, YH Liu, MQ Jia, QG Liu… - Bioorganic …, 2023 - Elsevier
In this study, twenty-one novel 2, 4-diaminopyrimidine cinnamyl derivatives as inhibitors
targeting FAK were designed and synthesized based on the structure of TAE-226, and the …