ArticleMolecules (Basel, Switzerland)2025
Synthesis and Anti-Tumor Evaluation of Carboranyl BMS-202 Analogues-A Case of Carborane Not as Phenyl Ring Mimetic.
Article in Molecules (Basel, Switzerland), 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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15 authors.
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Abstract
Carborane is considered a three-dimensional mimetic of phenyl rings in medicinal chemistry. BMS-202 is a potent PD-L1 inhibitor that can block the PD-L1/PD-1 interaction and restore the immune response to cancer cells. Herein, we replaced the terminal phenyl group of BMS-202 with carborane and prepared its carboranyl BMS-202 analogues. The results showed a loss of PD-L1 binding affinity due to the bulky size of carborane, suggesting that carborane cannot serve as a phenyl ring mimetic in certain cases. Docking study demonstrated that the narrow binding pocket of PD-L1 could not hold the bulky carborane, resulting in loss of its activity. Compounds
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