111423-01-9

Upstream product

• 16078-71-0 ethyl 5-amino-1-phenyl-1H-pyrazole-4-carboxylate 
• 701-73-5 methyl N-phenyldithiocarbamate 
• 62-53-3 aniline 
• 198716-01-7 1-Phenyl-6-thioxo-6,7-dihydro-1H-pyrazolo[3,4-d][1,3]thiazin-4-one 
• 58046-54-1 5-amino-1-phenyl-1H-pyrazole-4-carbohydrazide 
• 110810-00-9 5-Amino-1-phenyl-1H-pyrazole-4-carboxylic acid [1-phenyl-meth-(E)-ylidene]-hydrazide 
• 198715-89-8 5-Amino-1-phenyl-1H-pyrazole-4-carboxylic acid [1-(4-chloro-phenyl)-meth-(Z)-ylidene]-hydrazide 
• 198715-88-7 5-Amino-1-phenyl-1H-pyrazole-4-carboxylic acid [1-(4-methoxy-phenyl)-meth-(Z)-ylidene]-hydrazide 
• 100-63-0 phenylhydrazine 
• 103-72-0 phenyl isothiocyanate 

Downstream Products

• 113269-23-1 1-Phenyl-1H-9-thia-1,2,4a,10-tetraaza-cyclopenta[b]fluoren-4-one 
• 1152689-66-1 6-hydrazinyl-1,5-diphenyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one 

Relevant academic research and scientific papers

Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line

Some novel 6-substituted pyrazolo[3,4-d]pyrimidines 4, 5, 6a-d, 7a-c, 8 and pyrazolo[4,3-e][1,2,4]triazolo[4,3-a]pyrimidines 9a-c, 10a-c, 11, 12a,b, 13a-c and 14 were synthesized and characterized by spectral and elemental analyses. They were screened for their biological activity in?vitro against Abl and Src kinases. Compounds 7a and 7b revealed the highest activity against both wild and mutant Abl kinases as well as the Src kinase and the leukemia K-562?cell line. They can be considered as new hits for further structural optimization to obtain better activity.

Novel 1,5-diphenyl-6-substituted 1H-pyrazolo[3,4-d]pyrimidin-4(5H)-ones induced apoptosis in RKO colon cancer cells

Novel 1,5-diphenyl-6-substituted-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-ones were synthesized and characterized. All compounds were screened for their anti-proliferative activities in five different cancer cell lines. The results showed that compounds 7a and 7b comprising aminoguanidino or guanidino moiety at position 6 inhibited proliferation of RKO colon cancer cells with IC50 of 8 and 4 μM, respectively. Compounds 7a and 7b induced apoptosis in RKO cells, which was confirmed by TUNEL and annexin V-FITC assays. Flow cytometric analysis indicated that compounds 7a and 7b arrested RKO cells in the G1 phase and the most active compound 7b increased levels of p53, p21, Bax, ERK1/2 and reduced levels of Bcl2 and Akt. Compound 7b also activates release of cytochrome c, which is consistent with activation of caspase-9. Additionally, compound 7b increased caspase-3 activity and cleaved PARP-1 in RKO cells. Collectively, these findings could establish a molecular basis for the development of new anti-cancer agents.

Syntheis of Some New Pyrazolotriazines, Pyrazolothiazines and Pyrazolopyrimidines

When the pyrazole derivatives 3a,b were treated with triethyl orthoformate, the pyrazolotriazinethiones 5a,b were obtained.These were S-alkylated to give compounds 6a-d.Treatment of 5a,b with hydrazine hydrate in ethanol afforded 7,8 respectively.Benzylid

METHYL N-ARYLDITHIOCARBAMATES: USEFUL REAGENTS FOR THE ANNELATION OF PYRIMIDINES AND 1,3-OXAZINES TO FIVE-MEMBERED HETEROCYCLIC RINGS

The reaction of methyl N-aryldithiocarbamates with ?-excessive heteroaromatic o-amino acid derivatives leads to the annelation of 4-oxo-2-thioxopyrimidines, 2,4-dioxopyrimidines or 2-arylamino-1,3-oxazines, depending on the reaction conditions.