1092506-65-4Relevant articles and documents
Rh(III)-catalyzed C-H activation and double directing group strategy for the regioselective synthesis of naphthyridinones
Huckins, John R.,Bercot, Eric A.,Thiel, Oliver R.,Hwang, Tsang-Lin,Bio, Matthew M.
, p. 14492 - 14495 (2013)
A general Rh(III)-catalyzed synthesis of naphthyridinone derivatives is described. It relies on a double-activation and directing approach leveraging nicotinamide N-oxides as substrates. In general, high yields and selectivities can be achieved using low
Hemozoin inhibiting 2-phenylbenzimidazoles active against malaria parasites
L'abbate, Fabrizio P.,Müller, Ronel,Openshaw, Roxanne,Combrinck, Jill M.,de Villiers, Katherine A.,Hunter, Roger,Egan, Timothy J.
, p. 243 - 254 (2018/10/15)
The 2-phenylbenzimidazole scaffold has recently been discovered to inhibit β-hematin (synthetic hemozoin) formation by high throughput screening. Here, a library of 325,728 N-4-(1H-benzo[d]imidazol-2-yl)aryl)benzamides was enumerated, and Bayesian statistics used to predict β-hematin and Plasmodium falciparum growth inhibition. Filtering predicted inactives and compounds with negligible aqueous solubility reduced the library to 35,124. Further narrowing to compounds with terminal aryl ring substituents only, reduced the library to 18, 83% of which were found to inhibit β-hematin formation 100 μM and 50% parasite growth 2 μM. Four compounds showed nanomolar parasite growth inhibition activities, no cross-resistance in a chloroquine resistant strain and low cytotoxicity. QSAR analysis showed a strong association of parasite growth inhibition with inhibition of β-hematin formation and the most active compound inhibited hemozoin formation in P. falciparum, with consequent increasing exchangeable heme. Pioneering use of molecular docking for this system demonstrated predictive ability and could rationalize observed structure activity trends.
NOVEL PHENYLAMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF BCR-ABL KINASE
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Page/Page column 39, (2008/06/13)
The present invention relates to novel intermediates useful for the preparation of novel phenylaminopyrimidine derivatives, novel phenylaminopyrimidine derivatives. Pharmaceutical composition containing the novel phenylaminopyrimidine derivatives and processes for their preparation. The invention particularly relates to novel Phenyl pyrimidine amine derivatives of the general formula (I). The novel compounds of the formula 1 can be used in the therapy of Chronic Myeloid Leukemia (CML). Since the IC50; 191 values of these molecules are in the range 0.1 to 10.0 nm, these novel compounds are potentially useful for the treatment of CML.
