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-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