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Open access Sep 2026

Engineering a Redox-Responsive Bimolecular Prodrug for Targeted Gastric Cancer Combination Therapy: Design, Synthesis, and In Vivo Evaluation

Combination chemotherapy often suffers from asynchronous pharmacokinetics and off-target toxicity. To address this, we designed a novel, unreported engineered prodrug—a redox-responsive bimolecular prodrug (CA-4-Gefitinib)—by engineering a disulfide bond as a cleavable linker to covalently conjugate the tubulin inhibit...

Chao Wang, Yu-Tao Xiu, Yu-Jing Zhang et al. · 0 citations
Sep 2026

Discovery of a Novel HDAC1 Inhibitor to Potentiate Ferroptosis with Arachidonic Acid in ESCC

Ferroptosis represents a promising therapeutic strategy for esophageal squamous cell carcinoma (ESCC), but its efficacy is often limited by intrinsic metabolic defenses. Herein, arachidonic acid (AA) acts as a potent sensitizer for class I histone deacetylase (HDAC) inhibitor-induced ferroptosis. Guided by the bindin...

Meng Liu, Shan Gao, Chen Chen et al. · 0 citations
Open access Aug 2026

Conformationally constrained 6‑aryl‑1‑(3,4,5‑trimethoxyphenyl)-1H-pyrazolo[3,4‑b]pyrazines as novel microtubule destabilizers: design, synthesis, and antitumor evaluation

Findings establish the pyrazolo[3,4‑b]pyrazine scaffold as a promising platform for microtubule‑targeting anticancer agents and identify 10t as a compelling lead for further development.

Zhu Guo, Yu-Jing Zhang, Ping Zou et al. · 0 citations
Open access Aug 2026

Novel 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine derivatives: design, synthesis, and biological evaluation as potent tubulin polymerisation inhibitors with anticancer activity

Mechanistic assays confirmed 9t serves as a promising dual-function tubulin inhibitor with both cytostatic and cytotoxic anticancer effects, meriting further preclinical investigation.

Jia-Ke Gao, Yu-Jing Zhang, Rui Qu et al. · 0 citations

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