Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: The discovery of AZD8055 and AZD2014 was written by Pike, Kurt G.;Malagu, Karine;Hummersone, Marc G.;Menear, Keith A.;Duggan, Heather M. E.;Gomez, Sylvie;Martin, Niall M. B.;Ruston, Linette;Pass, Sarah L.;Pass, Martin. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2013.Product Details of 938443-20-0 This article mentions the following:
The optimization of a potent and highly selective series of dual mTORC1 and mTORC2 inhibitors is described. An initial focus on improving cellular potency while maintaining or improving other key parameters, such as aqueous solubility and margins over hERG IC50, led to the discovery of the clin. candidate AZD8055. Further optimization, particularly aimed at reducing the rate of metabolism in human hepatocyte incubations, resulted in the discovery of the clin. candidate AZD2014. In the experiment, the researchers used many compounds, for example, 2,4,7-Trichloropyrido[2,3-d]pyrimidine (cas: 938443-20-0Product Details of 938443-20-0).
2,4,7-Trichloropyrido[2,3-d]pyrimidine (cas: 938443-20-0) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Product Details of 938443-20-0
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia