34068-01-4Relevant articles and documents
Transition-Metal-Free and Base-Promoted Carbon-Heteroatom Bond Formation via C-N Cleavage of Benzyl Ammonium Salts
Liu, Long,Tang, Yuanyuan,Wang, Kunyu,Huang, Tianzeng,Chen, Tieqiao
, p. 4159 - 4170 (2021/03/09)
A facile and general method for constructing carbon-heteroatom (C-P, C-O, C-S, and C-N) bonds via C-N cleavage of benzyl ammonium salts under transition-metal-free conditions was reported. The combination of t-BuOK and 18-crown-6 enabled a wide range of substituted benzyl ammonium salts to couple readily with different kinds of heteroatom nucleophiles, i.e. hydrogen phosphoryl compounds, alcohols, thiols, and amines. Good functional group tolerance was demonstrated. The scale-up reaction and one-pot synthesis were also successfully performed.
ANTIVIRAL 1,3-DI-OXO-INDENE COMPOUNDS
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Paragraph 0401, (2021/10/22)
The invention provides compounds of Formula (I): as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections.
Optimization of ether and aniline based inhibitors of lactate dehydrogenase
Christov, Plamen P.,Kim, Kwangho,Jana, Somnath,Romaine, Ian M.,Rai, Ganesha,Mott, Bryan T.,Allweil, Alexander A.,Lamers, Alexander,Brimacombe, Kyle R.,Urban, Daniel J.,Lee, Tobie D.,Hu, Xin,Lukacs, Christine M.,Davies, Douglas R.,Jadhav, Ajit,Hall, Matthew D.,Green, Neal,Moore, William J.,Stott, Gordon M.,Flint, Andrew J.,Maloney, David J.,Sulikowski, Gary A.,Waterson, Alex G.
supporting information, (2021/04/12)
Lactate dehydrogenase (LDH) is a critical enzyme in the glycolytic metabolism pathway that is used by many tumor cells. Inhibitors of LDH may be expected to inhibit the metabolic processes in cancer cells and thus selectively delay or inhibit growth in transformed versus normal cells. We have previously disclosed a pyrazole-based series of potent LDH inhibitors with long residence times on the enzyme. Here, we report the elaboration of a new subseries of LDH inhibitors based on those leads. These new compounds potently inhibit both LDHA and LDHB enzymes, and inhibit lactate production in cancer cell lines.