926907-33-7Relevant academic research and scientific papers
3-HYDROXYISOTHIAZOLE-4-CARBOXAMIDINE DERIVATIVES AS CHK2 INHIBITORS
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Page/Page column 11-12, (2009/01/23)
This invention provides compounds of Formula (I), which are inhibitors of Chk2 and are useful as a radiation protection agents in anticancer radiotherapy. A method of modulating Chk2 in vitro includes treating a substrate with Chk2 in the presence of compounds of formula I. A method of making a compound of formula I includes: a) forming a biaryl amine having an amino (NH2) group; b) converting the amino group to an isothiocyanate group; c) adding a cyanoacetamide to said isothiocyanate group to form a thioamide adduct; d) cyclizing said thioamide adduct to form an isothiazole having a cyano group; and e) adding an amine to said cyano group to form a carboxamidine group.
Identification of novel, selective and potent Chk2 inhibitors
Larson, Gary,Yan, Shunqi,Chen, Huanming,Rong, Frank,Hong, Zhi,Wu, Jim Zhen
, p. 172 - 175 (2007/10/03)
A series of isothiazole carboxamidine compounds were synthesized and discovered as novel and selective inhibitors for Chk2. They are not active against the related Chk1 kinase. The structure-activity relationship studies were performed on the scaffold, an
