Topics
Treatment, Biology / Mechanism, Side effects / Toxicity
Modality
Targeted therapy, Imaging
Study type
Lab / Preclinical
Abstract
The development of dual-targeted inhibitors represents a promising strategy to address the challenges of drug resistance and limited efficacy in cancer therapy. This study describes the design, synthesis, and evaluation of novel inhibitors targeting VEGFR2 and HDAC through a structure-based pharmacophore-merging strategy. We integrated…
Authors
Yaxin Li, Sisi Liu, Sha Hu, Ranran Zhang +9
AI-generated summary
Structure-Based Design and Free Energy Perturbation-Guided Synthesis of Novel VEGFR2 and HDAC Dual Inhibitors with Potent Antitumor Efficacy. reports: The development of dual-targeted inhibitors represents a promising strategy to address the challenges of drug resistance and limited efficacy in cancer therapy. This study describes the design, synthesis, and evaluation of novel inhibitors targeting VEGFR2 and HDAC through a structure-based pharmacophore-merging strategy. We integrated the hydroxamic acid zinc-binding group and the linker into the back pocket of VEGFR2.
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Primary source: PubMed.