547739-67-3Relevant articles and documents
Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent
Brachet, Etienne,Dumond, Aurore,Liu, Wang-Qing,Fabre, Marie,Selkti, Mohamed,Raynaud, Fran?oise,Hermine, Olivier,Benhida, Rachid,Belmont, Philippe,Garbay, Christiane,Lepelletier, Yves,Ronco, Cyril,Pagès, Gilles,Demange, Luc
supporting information, (2019/11/21)
We report herein the synthesis of a newly described anti-cancer agent, NRPa-308. This compound antagonizes Neuropilin-1, a multi-partners transmembrane receptor overexpressed in numerous tumors, and thereby validated as promising target in oncology. The p
Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A
Patrone, James D.,Pelz, Nicholas F.,Bates, Brittney S.,Souza-Fagundes, Elaine M.,Vangamudi, Bhavatarini,Camper, Demarco V.,Kuznetsov, Alexey G.,Browning, Carrie F.,Feldkamp, Michael D.,Frank, Andreas O.,Gilston, Benjamin A.,Olejniczak, Edward T.,Rossanese, Olivia W.,Waterson, Alex G.,Chazin, Walter J.,Fesik, Stephen W.
supporting information, p. 893 - 899 (2016/05/09)
Replication protein A (RPA) is an essential single-stranded DNA (ssDNA)-binding protein that initiates the DNA damage response pathway through protein-protein interactions (PPIs) mediated by its 70N domain. The identification and use of chemical probes that can specifically disrupt these interactions is important for validating RPA as a cancer target. A high-throughput screen (HTS) to identify new chemical entities was conducted, and 90 hit compounds were identified. From these initial hits, an anthranilic acid based series was optimized by using a structure-guided iterative medicinal chemistry approach to yield a cell-penetrant compound that binds to RPA70N with an affinity of 812 nm. This compound, 2-(3- (N-(3,4-dichlorophenyl)sulfamoyl)-4-methylbenzamido)benzoic acid (20 c), is capable of inhibiting PPIs mediated by this domain.
INHIBITOR OF NEUROPILIN AND USE THEREOF FOR THE TREATMENT OF NEUROPILIN-RELATED DISEASES
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Page/Page column 34, (2015/02/02)
The present invention relates to a compound of general formula (I), and salts or solvate thereof, for treating a Neuropilin-related disease, disorder or condition; and to a composition, a pharmaceutical composition and a medicament comprising the compound of general formula (I).
