Current evidence suggests that enhanced CDK4 selectivity and rational combination strategies may improve the therapeutic index in NSCLC and coumarin-based scaffolds are promising platforms for CDK4-targeted drug development.
Repurposing of existing drugs has emerged as a time- and cost-effective strategy in oncology drug discovery. Given the critical role of dysregulated kinase signaling in cancer, kinase-focused repurposing strategies have attracted considerable interest. This approach encompasses both “target hopping” between different k...
This review critically evaluates recent advances in indole-based anticancer agents, with particular emphasis on structure–activity relationships (SAR), molecular mechanisms, and target-oriented drug design.
Aashik Malik, Mayank Yadav, J. Kadian et al.· Medicinal Chemistry Research· 0 citations
This review analyzes recent Akt inhibitors, with particular focus on the structure–activity relationship (SAR) of their heterocyclic core scaffolds and the resulting biological activity.
Mayur S. Dhangar, Mahesh B. Palkar· Chemistry and Biodiversity· 0 citations
Findings support nilotinib as a promising therapeutic candidate for KRAS-mutant NSCLC after a structure-based drug repurposing approach was employed to screen FDA-approved compounds targeting key regulators to the MAPK signalling pathway.
Anisha Jain, Chandan Dharmashekar, B. S et al.· Scientific Reports· 0 citations
G856-6814 is supported as a NAT10-targeting inhibitory scaffold that requires broader selectivity and in vivo evaluation and attenuation of cellular effects after NAT10 knockdown.
Chao Xu, Shi-Lei Zhao, Bing Xu et al.· Journal of Computer-Aided Mo...· 0 citations
A structure–activity relationship (SAR)-guided strategy was employed to identify novel coumarin-based HDAC2 inhibitors, highlighting the coumarin scaffold, an additional aromatic ring, a 3–6 atom linker, a furan bridge, and terminal hydroxyl or methoxy groups as key structural features.
Amrita Singh, Deepak Singh· Main group chemistry (Print)· 0 citations
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