Extracurricular laboratory:new discovery of 39093-93-1

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39093-93-1, Name is Thiomorpholine 1,1-dioxide, belongs to Thiomorpholine compound, is a common compound. Quality Control of Thiomorpholine 1,1-dioxideIn an article, once mentioned the new application about 39093-93-1.

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors

Taking the pyrrolopyrimidine derived IGF-1R inhibitor NVP-AEW541 as the starting point, the benzyl ether back-pocket binding moiety was replaced with a series of 2-cyclic ether methyl ethers leading to the identification of novel achiral [2.2.1]-bicyclic ether methyl ether containing analogues with improved IGF-1R activities and kinase selectivities. Further exploration of the series, including a fluorine scan of the 5-phenyl substituent, and optimisation of the sugar-pocket binding moiety identified compound 33 containing (S)-2-tetrahydrofuran methyl ether 6-fluorophenyl ether back-pocket, and cis-N-Ac-Pip sugar-pocket binding groups. Compound 33 showed improved selectivity and pharmacokinetics compared to NVP-AEW541, and produced comparable in vivo efficacy to linsitinib in inhibiting the growth of an IGF-1R dependent tumour xenograft model in the mouse.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 39093-93-1, help many people in the next few years.Quality Control of Thiomorpholine 1,1-dioxide

Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem