2631-61-0Relevant articles and documents
Naphthyl ketones: A new class of Janus kinase 3 inhibitors
Brown, George R.,Bamford, Andrea M.,Bowyer, Jonathan,James, Daniel S.,Rankine, Neil,Tang, Eric,Torr, Vanessa,Culbert, Eric J.
, p. 575 - 579 (2000)
Potent inhibition of Janus kinase 3 was found for a series of naphthyl(β-aminoethyl)ketones (e.g. 7, pIC50 = 7.1 ± 0.3). Further studies indicated that these compounds fragment in less than 1 h by retro-Michael reaction in the Jak3 in vitro ELISA assay procedure. The breakdown product of 7,2-naphthylvinyl ketone (22, pIC50 = 6.8 ± 0.3) showed very similar inhibitory activity to 7. Compounds 7 (in neutral buffer) and 22 will be useful pharmacological tools for the investigation of the Janus tyrosine kinase Jak3. (C) 2000 Elsevier Science Ltd. All rights reserved.
Stereoselective Construction of γ-Lactams via Copper-Catalyzed Borylacylation
Bajohr, Jonathan,Lautens, Mark,Polishchuk, Iuliia,Torelli, Alexa,Whyte, Andrew
supporting information, p. 7915 - 7919 (2020/11/02)
A versatile and highly stereoselective borylative cyclization to generate polyfunctionalized γ-lactams has been developed. The stereoselective synthesis of these key ring systems is crucial due to their ubiquity in natural products. We report the diastero- and enantioselective construction of di- and trisubstituted γ-lactam cores, with examples containing an enantioenriched quaternary carbon.
Pt coordination compound containing quinazoline ligands as well as preparation method and application of Pt coordination compound
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Paragraph 0095; 0097, (2017/06/02)
The invention relates to a Pt coordination compound containing quinazoline ligands. The Pt coordination compound is expressed in a general formula [Pt(XYZ)C]B,wherein XYZ is tridentate provided in a formula (1a) or (1b); and C is a monodentate prov
Synthesis and anti-tubercular activity of conformationally-constrained and bisquinoline analogs of TMC207
Kalia, Dimpy,Anil Kumar,Meena, Gajanand,Sethi, Kashmir Prasad,Sharma, Rohit,Trivedi, Priyanka,Khan, Shaheb Raj,Verma, Ajay Singh,Singh, Shyam,Sharma, Sandeep,Roy, Kuldeep K.,Kant, Ruchir,Krishnan, Manju Yasodha,Singh, Bhupendra N.,Sinha, Sudhir,Chaturvedi, Vinita,Saxena, Anil K.,Dikshit, Dinesh K.
, p. 1554 - 1563 (2015/08/24)
One of the most significant breakthroughs in the battle against tuberculosis is the recent approval of the quinoline compound, TMC207, for the treatment of drug-resistant tuberculosis. To gain insight into the molecular determinants of the activity of TMC207 and to evaluate the scope of quinoline compounds as anti-tubercular agents, we synthesized a series of TMC207 derivatives and evaluated their anti-tubercular activity. Making the lateral chain of the drug rigid by linking it to an adjacent phenyl substituent resulted in a decrease in activity. In contrast, replacing a phenyl substituent of TMC207 with a quinoline moiety gave bisquinolines that demonstrated potent anti-tubercular activity in in vitro experiments, in ex vivo mouse bone marrow macrophage assays, and also in the in vivo mouse model of the disease. These results provide new guiding principles for modifying the TMC207 scaffold to develop efficacious anti-tubercular drugs and set the stage for the development of bisquinolines as a promising new class of anti-tubercular agents.