877212-94-7

Basic information

• Product Name: 2,5-Diazabicyclo[2.2.1]heptane-2-carboxylic acid, 5-(4-nitrophenyl)-, 1,1-dimethylethyl ester
• CAS NO: 877212-94-7
• Molecular Formula: C16H21N3O4
• Molecular Weight: 319.36
• Mol File: 877212-94-7.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: 2,5-Diazabicyclo[2.2.1]heptane-2-carboxylic acid, 5-(4-nitrophenyl)-, 1,1-dimethylethyl ester(CAS DataBase Reference)
• NIST Chemistry Reference: 2,5-Diazabicyclo[2.2.1]heptane-2-carboxylic acid, 5-(4-nitrophenyl)-, 1,1-dimethylethyl ester(877212-94-7)
• EPA Substance Registry System: 2,5-Diazabicyclo[2.2.1]heptane-2-carboxylic acid, 5-(4-nitrophenyl)-, 1,1-dimethylethyl ester(877212-94-7)

Safety Data

• Hazardous Substances Data: 877212-94-7(Hazardous Substances Data)

Upstream product

• 350-46-9 4-Fluoronitrobenzene 
• 198989-07-0 tert-butyl 2,5-diazabicyclo[2.2.1]heptane-2-carboxylate 

Downstream Products

• 1093094-99-5 5-(4-nitrophenyl)-2,5-diazabicyclo[2.2.1]heptane 
• 643087-74-5 5-(4-aminophenyl)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester 

Relevant articles and documents

Design and synthesis of 4-(Heterocyclic substituted amino)-1h-pyrazole-3-carboxamide derivatives and their potent activity against acute myeloid leukemia (AML)

Fms-like receptor tyrosine kinase 3 (FLT3) has been emerging as an attractive target for the treatment of acute myeloid leukemia (AML). By modifying the structure of FN-1501, a potent FLT3 inhibitor, 24 novel 1H-pyrazole-3-carboxamide derivatives were designed and synthesized. Compound 8t showed strong activity against FLT3 (IC50: 0.089 nM) and CDK2/4 (IC50: 0.719/0.770 nM), which is more efficient than FN-1501(FLT3, IC50: 2.33 nM; CDK2/4, IC50: 1.02/0.39 nM). Compound 8t also showed excellent inhibitory activity against a variety of FLT3 mutants (IC50 50: 1.22 nM). In addition, compound 8t significantly inhibited the proliferation of most human cell lines of NCI60 (GI50 1 μM for most cell lines). Taken together, these results demonstrated the potential of 8t as a novel compound for further development into a kinase inhibitor applied in cancer therapeutics.

INDOLINONE DERIVATIVES AND THEIR USE IN TREATING DISEASE-STATES SUCH AS CANCER

The present invention encompasses compounds of general formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.