960225-75-6Relevant articles and documents
HETEROCYCLIC COMPOUND
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Paragraph 0329, (2018/03/25)
The present invention relates to a compound which can be useful for the treatment or prevention of SPT-related diseases including cancer and congenital diseases associated with sphingolipid accumulation (including Niemann-Pick disease).
Development of small-molecule probes that selectively kill cells induced to express mutant RAS
We?wer, Michel,Bittker, Joshua A.,Lewis, Timothy A.,Shimada, Kenichi,Yang, Wan Seok,MacPherson, Lawrence,Dandapani, Sivaraman,Palmer, Michelle,Stockwell, Brent R.,Schreiber, Stuart L.,Munoz, Benito
supporting information; experimental part, p. 1822 - 1826 (2012/04/04)
Synthetic lethal screening is a chemical biology approach to identify small molecules that selectively kill oncogene-expressing cell lines with the goal of identifying pathways that provide specific targets against cancer cells. We performed a high-throughput screen of 303,282 compounds from the National Institutes of Health-Molecular Libraries Small Molecule Repository (NIH-MLSMR) against immortalized BJ fibroblasts expressing HRASG12V followed by a counterscreen of lethal compounds in a series of isogenic cells lacking the HRASG12V oncogene. This effort led to the identification of two novel molecular probes (PubChem CID 3689413, ML162 and CID 49766530, ML210) with nanomolar potencies and 4-23-fold selectivities, which can potentially be used for identifying oncogene-specific pathways and targets in cancer cells.
Kinetics of hydrolysis of five-membered C-nitroheterocycles: Pyrazole, imidazole, 1,2,4-triazole, and isoxazole derivatives
Trukhacheva,Levina,Grigor'ev,Arzamastsev,Dalinger,Vatsadze,Popova,Shevelev,Granik
, p. 2813 - 2819 (2007/10/03)
Alkaline hydrolysis of mono-and dinitro derivatives of five-membered heterocycles, viz., pyrazole, imidazole, 1,2,4-triazole, and isoxazole, is accompanied by the elimination of the nitro group in the form of a nitrite anion. The hydrolysis kinetics was studied by the polarographic and photometric methods. The experimentally determined hydrolysis rate constants depend on the nature of the heterocycle. A possible mechanism for hydrolytic transformations of the compounds under study was proposed on the basis of the calculated thermodynamic parameters of the reaction (Δ G ≠, ΔH ≠, ΔS ≠).
