Fragment‐Based Design, Synthesis, and Biological Evaluation of 1‐Substituted‐indole‐2‐carboxylic Acids as Selective Mcl‐1 Inhibitors
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DOI: 10.1002/ardp.201600251
Abstract: Based on a known selective Mcl‐1 inhibitor, 6‐chloro‐3‐(3‐(4‐chloro‐3,5‐dimethylphenoxy)propyl)‐1H‐indole‐2‐carboxylic acid, we applied a fragment‐based approach to obtain new molecules that extended into the p1 pocket of the BH3 groove and then exhibited binding selectivity for the… read more here.
Keywords: mcl; indole carboxylic; selective mcl; fragment based ... See more keywords
Structure‐Atropisomer Stability Relationship in Selective MCL‐1 Inhibitors
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DOI: 10.1002/cmdc.202400970
Abstract: Atropisomersm is an emerging feature in recent drug candidates due to the increasing complexity of the targeted protein surfaces. The developability of the drug candidates requires that their atropisomer interconversion is either fast or very… read more here.
Keywords: selective mcl; stability; mcl inhibitors; structure atropisomer ... See more keywords
Structure-Based Optimization of 3-Phenyl-N-(2-(3-phenylureido)ethyl)thiophene-2-sulfonamide Derivatives as Selective Mcl-1 Inhibitors.
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DOI: 10.1021/acs.jmedchem.1c00690
Abstract: Selective Mcl-1 inhibitors may overcome the drug resistance caused by current anti-apoptotic Bcl-2 protein inhibitors in tumors with Mcl-1 overexpression. Based on previously discovered compounds with a 3-phenylthiophene-2-sulfonamide core moiety, in this work, we have… read more here.
Keywords: optimization phenyl; mcl inhibitors; selective mcl; based optimization ... See more keywords