72373-81-0Relevant articles and documents
WDR5-MYC INHIBITORS
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Paragraph 00515; 00924-00925, (2021/02/05)
Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction
Macdonald, Jonathan D.,Chacón Simon, Selena,Han, Changho,Wang, Feng,Shaw, J. Grace,Howes, Jennifer E.,Sai, Jiqing,Yuh, Joannes P.,Camper, Demarco,Alicie, Bethany M.,Alvarado, Joseph,Nikhar, Sameer,Payne, William,Aho, Erin R.,Bauer, Joshua A.,Zhao, Bin,Phan, Jason,Thomas, Lance R.,Rossanese, Olivia W.,Tansey, William P.,Waterson, Alex G.,Stauffer, Shaun R.,Fesik, Stephen W.
, p. 11232 - 11259 (2019/12/25)
The treatment of tumors driven by overexpression or amplification of MYC oncogenes remains a significant challenge in drug discovery. Here, we present a new strategy toward the inhibition of MYC via the disruption of the protein-protein interaction betwee
Two Routes to 4-Fluorobenzisoxazol-3-one in the Synthesis of a 5-HT4 Partial Agonist
Widlicka, Daniel W.,Murray, John C.,Coffman, Karen J.,Xiao, Chunguang,Brodney, Michael A.,Rainville, Joseph P.,Samas, Brian
, p. 233 - 241 (2016/03/04)
A potent 5-HT4 partial agonist, 1 (PF-04995274), targeted for the treatment of Alzheimer's disease and cognitive impairment, has been prepared on a multi-kilogram scale. The initial synthetic route, that proceeded through a 4-substituted 3-hydroxybenzisoxazole core, gave an undesired benzoxazolinone through a Lossen-type rearrangement. Route scouting led to two new robust routes to the desired 4-substituted core. Process development led to the efficient assembly of the API on a pilot plant scale under process-friendly conditions with enhanced throughput. In addition, crystallization of a hemicitrate salt of the API with pharmaceutically beneficial properties was developed to enable progression of clinical studies.