Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent was written by Liu, Yong;Laufer, Radoslaw;Patel, Narendra Kumar;Ng, Grace;Sampson, Peter B.;Li, Sze-Wan;Lang, Yunhui;Feher, Miklos;Brokx, Richard;Beletskaya, Irina;Hodgson, Richard;Plotnikova, Olga;Awrey, Donald E.;Qiu, Wei;Chirgadze, Nickolay Y.;Mason, Jacqueline M.;Wei, Xin;Lin, Dan Chi-Chia;Che, Yi;Kiarash, Reza;Fletcher, Graham C.;Mak, Tak W.;Bray, Mark R.;Pauls, Henry W.. And the article was included in ACS Medicinal Chemistry Letters in 2016.Application of 5856-63-3 This article mentions the following:
This work describes a scaffold hopping exercise that begins with known imidazo[1,2-a]pyrazines, briefly explores pyrazolo[1,5-a][1,3,5]triazines, and ultimately yields pyrazolo[1,5-a]pyrimidines as a novel class of potent TTK inhibitors. An X-ray structure of a representative compound is consistent with 11/2 type inhibition and provides structural insight to aid subsequent optimization of in vitro activity and physicochem. and pharmacokinetic properties. Incorporation of polar moieties in the hydrophobic and solvent accessible regions modulates physicochem. properties while maintaining potency. Compounds with enhanced oral exposure were identified for xenograft studies. The work culminates in the identification of a potent (TTK Ki = 0.1 nM), highly selective, orally bioavailable anticancer agent (CFI-402257) for IND enabling studies. In the experiment, the researchers used many compounds, for example, (R)-2-Aminobutan-1-ol (cas: 5856-63-3Application of 5856-63-3).
(R)-2-Aminobutan-1-ol (cas: 5856-63-3) belongs to alcohols. Similar to water, an alcohol can be pictured as having an sp3 hybridized tetrahedral oxygen atom with nonbonding pairs of electrons occupying two of the four sp3 hybrid orbitals. Secondary alcohols are easily oxidized without breaking carbon-carbon bonds only as far as the ketone stage. No further oxidation is seen except under very stringent conditions.Application of 5856-63-3
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts