Results 131 to 140 of about 42,319 (209)

Design and Evaluation of Bivalent K‐Ras Inhibitors That Target the CAAX Binding Site and the Acidic Surface of Farnesyltransferase and Geranylgeranyltransferase I

open access: yesChemistry – A European Journal, Volume 31, Issue 27, May 14, 2025.
Chemical inhibition of K‐Ras posttranslational prenylation represents a promising strategy against aggressive cancers. A structure‐based design produces piperidine‐based peptidomimetics conjugated to cationic modules, effectively inhibiting FTase and GGTase I at single‐digit nanomolar concentrations.
Naomi Horiuchi   +8 more
wiley   +1 more source

Design and Synthesis of Tetrahydropyrrolo[3,4‐c]Pyrazole Sigma‐1 Receptor Ligands

open access: yesChemMedChem, Volume 20, Issue 9, May 5, 2025.
This study highlights the tetrahydropyrrolo[3,4‐c]pyrazole scaffold as a promising platform for S1R ligands development. Key findings include compound 19’s high S1R affinity (Ki=75 nM), influenced by strategic nitrogen substitutions and reduced steric hindrance.
Giuseppe Cosentino   +7 more
wiley   +1 more source

Design, synthesis, and investigation of novel 5-arylpyrazole-glucose hybrids as α-glucosidase inhibitors. [PDF]

open access: yesSci Rep
Hariri R   +9 more
europepmc   +1 more source

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