59815-29-1Relevant academic research and scientific papers
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.
COMPOUNDS FORTREATMENT OF CARDIOVASCULAR DISEASES
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Page/Page column 41, (2008/06/13)
Pharmaceutical compositions containing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors in combination with Ca 2+ overload inhibitors, and the use of such combination inhibitors to treat, for example, cardiovascular disease, such as ischemia, particularly, perioperative myocardial ischemic injury in mammals, including humans, are disclosed.
Synthesis of the highly selective Na+/H+ exchange inhibitors cariporide mesilate and (3-methanesulfonyl-4-piperidino-benzoyl) guanidine methanesulfonate
Weichert, Andreas,Faber, Sabine,Jansen, Hans W.,Scholz, Wolfgang,Lang, Hans J.
, p. 1204 - 1207 (2007/10/03)
The syntheses of cariporide mesilate ((4-isopropyl-3-methanesulfonyl-benzoyl) guanidine methanesulfonate, HOE 642, CAS 159138-81-5), currently being clinically investigated as a protective drug in cardiac ischemia and reperfusion states, and of HOE 694 ((3-methanesulfonyl-4-piperidino-benzoyl)guanidine methanesulfonate, CAS 149725-40-6), widely used as a physiological and pharmacological research tool in studies comprising Na+/H+ exchange (NHE) inhibition, are described. Additionally, their selectivity on the different subtypes is disclosed.
Benzoylguanidines, pharmaceutical composition containing them and treatment of arrthythmias therewith
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, (2008/06/13)
Benzoylguanidines, process for their preparation, their use as a medicament and medicament containing them. The invention relates to benzoylguanidines of the formula I STR1 where R(1) or R(2) is R(3)-S(O)n -- or R(4)R(5)N--O2 S-- and
