2224-67-1

Upstream product

• 3185-99-7 Methyl p-tolyl sulfone 

Downstream Products

• 1101118-48-2 N'-((5-cyanopyrazolo[1,5-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-(methylsulfonyl)benzenesulfonohydrazide 
• 1671-23-4 5-Methylsulfonyl-2-methyl-benzolsulfonsaeure-⁽¹⁾-benzylamid 
• 2124-63-2 5-Methylsulfonyl-2-methyl-benzolsulfonsaeure-⁽¹⁾-methylamid 
• 1671-24-5 5-Methylsulfonyl-2-methyl-benzol-sulfonsaeure-⁽¹⁾-anilid 
• 1671-21-2 5-Methylsulfonyl-2-methyl-benzolsulfonsaeure-⁽¹⁾-ethylamid 
• 1671-20-1 Methyl-4-methyl-3-sulfamoylphenylsulfon 

Relevant academic research and scientific papers

Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR

Structure-activity relationship studies of the pyrazolo[1,5-a]pyridine class of PI3 kinase inhibitors show that substitution off the hydrazone nitrogen and replacement of the sulfonyl both gave a loss of p110α selectivity, with the exception of an N-hydroxyethyl analogue. Limited substitutions were tolerated around the phenyl ring; in particular the 2,5-substitution pattern was important for PI3 kinase activity. The N-hydroxyethyl compound also showed good inhibition of cell proliferation and inhibition of phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity. It had suitable pharmacokinetics for evaluation in vivo, and showed tumour growth inhibition in two human tumour cell lines in xenograft studies. This work has provided suggestions for the design of more soluble analogues.

PYRAZOLO[1,5-A]PYRIDINES AND THEIR USE IN CANCER THERAPY

Pyrazolo[1,5-a]pyridines are described, including methods for their preparation, and their use as agents or drugs for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.