629657-95-0

Upstream product

• 4774-14-5 2,6-dichloropyrazine 
• 56613-80-0 D-2-phenylglycinol 

Downstream Products

• 1617545-80-8 2-chloro-4-[6-((R)-2-hydroxy-1-phenyl-ethylamino)-pyrazin-2-yl]-phenol 
• 1617545-70-6 (R)-2-[6-(5-chloro-2-fluoro-phenyl)-pyrazin-2-ylamino]-2-phenyl-ethanol 
• 1617545-82-0 (R)-2-[6-(5-chloro-pyridin-3-yl)-pyrazin-2-ylamino]-2-phenyl-ethanol 
• 1617545-75-1 (R)-2-[6-(2-fluoro-4-hydroxyphenyl)-pyrazin-2-ylamino]-2-phenyl-ethanol 
• 1617545-84-2 (R)-2-[6-(3-chloro-phenyl)-pyrazin-2-ylamino]-2-phenyl-ethanol 
• 1617545-74-0 (R)-2-[6-(4-hydroxyphenyl)-pyrazin-2-ylamino]-2-phenyl-ethanol 

Relevant academic research and scientific papers

Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia

CDK9 is an essential drug target correlated to the development of acute myeloid leukemia (AML). Starting from the hit compound 10, which was discovered through a screening of our in-house compound library, the structural modifications were carried out based on the bioisosterism and scaffold hopping strategies. Consequently, compound 37 displayed the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM, which was nearly 1500-fold higher than compound 10. In addition, compound 37 exhibited significant antiproliferative activity in broad cancer cell lines. Further investigation of in vivo properties demonstrated that compound 37 could be orally administrated with an acceptable bioavailability (F = 33.7%). In MV-4-11 subcutaneous xenograft mouse model, compound 37 (7.5 mg/kg) could significantly suppress the tumor progression with a T/C value of 27.80%. Compound 37 represents a promising lead compound for the development of a novel class of CDK9 inhibitors for the treatment of acute myeloid leukemia.

NOVE PHENYL/PYRIDINE SERIES SUBSTITUED BY HYDROXYETHYLAMINO FOR THE TREATMENT OF CANCER

The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and W are as described herein, compositions including the compounds and methods of using the compounds.

PROTEIN KINASE INHIBITORS

A compound of general formula (I) or pharmaceutically acceptable salts, hydrates, solvates, crystal forms of diastereomers thereof is described. A method of treating protein kinase-associated disease states using the compound of Formula (I) is also described.