Discovery of Thiomorpholine 1,1-dioxide

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. 39093-93-1, In my other articles, you can also check out more blogs about 39093-93-1

Because a catalyst decreases the height of the energy barrier, 39093-93-1, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.39093-93-1, Name is Thiomorpholine 1,1-dioxide, molecular formula is C4H9NO2S. In a article£¬once mentioned of 39093-93-1

Structure-based design of 2,4-diaminopyrimidine derivatives bearing a pyrrolyl group as ALK and ROS1 inhibitors

In order to develop potent ALK and ROS1 dual inhibitors, twenty-eight 2,4-diaminopyrimidine derivatives (9a-9n and 10a-10n) bearing a pyrrolyl moiety were designed and synthesized based on the co-crystal structure of ceritinib with ALKwt protein. Most compounds displayed considerable activity against ALK and ROS1 addicted cells; meanwhile, compound 10d showed excellent activity against Karpas299, H2228 and HCC78 with IC50 values of 0.01, 0.08 and 0.042 muM. Subsequently, seven compounds were selected for kinase studies in vitro, resulting in the discovery of 10d with IC50 values of 1.8, 4.3 and 3.6 nM against ALK, ALKL1196M and ROS1, respectively. Furthermore, the biological assays revealed that compound 10d induced cell apoptosis in a dose-dependent manner. Ultimately, molecular docking studies presented reasonable and optimal binding interactions with ALKwt and ROS1.

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