TL;DR
The utility of integrated in silico methodologies in enabling the rational design of TRIM24-targeted agents for prostate cancer therapy is highlighted.
Tuberculosis (TB) remains a leading cause of infectious mortality worldwide, exacerbated by the emergence of multidrug-resistant strains and the dose-limiting toxicity of existing chemotherapeutics. Targeting regulatory mechanisms that potentiate current drugs offers a promising alternative strategy. EthR, a TetR-famil...
Abstract A new series of thiazole-based carboxamide derivatives (5–12) was designed, synthesized with structural elucidation performed using standard spectroscopic techniques including NMR and HRMS. The synthesized compounds were evaluated for their inhibitory activity against SARS-CoV-2 papain-like protease (PLpro) an...
Z4 more effectively inhibited proliferation and migration/invasion of BEL-7404 and HuH-7 cells than sorafenib, while inducing cell cycle arrest, mitochondrial dysfunction, reactive oxygen species (ROS) accumulation, and apoptosis, and provides a promising lead compound Z4 for anti-HCC drug discovery.
Findings support the Hydrazide–hydrazone derivatives' potential as EGFR kinase inhibitors, with M3 emerging as a particularly promising lead compound.
An integrated computational investigation of 44 hydrazide–hydrazone derivatives sharing a common 5H-chromen-5-one scaffold and evaluated for anticancer activity against HCT116 human colon carcinoma cells identifies S8 as a promising lead compound for further development as a potential anticancer agent targeting colorec...
A novel series of pyrazolo[1,5-a]pyrimidine derivatives was designed using ligand-based pharmacophore modeling, and their structures were confirmed by 1H/13C NMR and LC-MS, establishing 8a and 8i as potent, selective, and structurally stable lead candidates for preclinical COX-2 inhibitor development.
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