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...
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.· Journal of Medicinal Chemist...· 0 citations
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.· Journal of Enzyme Inhibition...· 0 citations
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.· Journal of Enzyme Inhibition...· 0 citations
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