1607005-09-3Relevant academic research and scientific papers
Creation of a Novel Class of Potent and Selective MutT Homologue 1 (MTH1) Inhibitors Using Fragment-Based Screening and Structure-Based Drug Design
Rahm, Fredrik,Viklund, Jenny,Trésaugues, Lionel,Ellermann, Manuel,Giese, Anja,Ericsson, Ulrika,Forsblom, Rickard,Ginman, Tobias,Günther, Judith,Hallberg, Kenth,Lindstr?m, Johan,Persson, Lars Boukharta,Silvander, Camilla,Talagas, Antoine,Díaz-Sáez, Laura,Fedorov, Oleg,Huber, Kilian V. M.,Panagakou, Ioanna,Siejka, Paulina,Gorjánácz, Mátyás,Bauser, Marcus,Andersson, Martin
, p. 2533 - 2551 (2018)
Recent literature has both suggested and questioned MTH1 as a novel cancer target. BAY-707 was just published as a target validation small molecule probe for assessing the effects of pharmacological inhibition of MTH1 on tumor cell survival, both in vitro and in vivo.(1) In this report, we describe the medicinal chemistry program creating BAY-707, where fragment-based methods were used to develop a series of highly potent and selective MTH1 inhibitors. Using structure-based drug design and rational medicinal chemistry approaches, the potency was increased over 10,000 times from the fragment starting point while maintaining high ligand efficiency and drug-like properties.
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Page/Page column 63; 64, (2014/05/24)
This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with exc
