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Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors
- Source :
- ACS Medicinal Chemistry Letters
- Publication Year :
- 2011
- Publisher :
- American Chemical Society, 2011.
-
Abstract
- A series of novel 3,5-diamino-1,2,4-triazole ben- zyl ureas was identified as having potent anaplastic lymphoma kinase (ALK) inhibition exemplified by 15a, 20a, and 23a, which exhibited antiproliferative IC50 values of 70, 40, and 20 nM in Tel-ALK transformed Ba/F3 cells, respectively. More- over, 15a and 23a potently inhibited the growth and survival of NPM-ALK positive anaplastic large cell lymphoma cell (SU- DHL-1) and neuroblastoma cell lines (KELLY, SH-SY5Y) containing the F1174L ALK mutation. These compounds provide novel leads for the development of small-molecule ALK inhibitors for cancer therapy.
- Subjects :
- Pathology
medicine.medical_specialty
Letter
Cell
Cancer therapy
medicine.disease_cause
Biochemistry
Neuroblastoma cell
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
hemic and lymphatic diseases
Drug Discovery
medicine
Ic50 values
Anaplastic lymphoma kinase
Anaplastic large-cell lymphoma
030304 developmental biology
0303 health sciences
Mutation
business.industry
Organic Chemistry
1,2,4-Triazole
medicine.disease
3. Good health
medicine.anatomical_structure
3,5-diamino-1,2,4-triazole urea
chemistry
ALK
030220 oncology & carcinogenesis
Cancer research
business
Subjects
Details
- Language :
- English
- ISSN :
- 19485875
- Volume :
- 2
- Issue :
- 5
- Database :
- OpenAIRE
- Journal :
- ACS Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....c97fe2e297dd7eef7d000655b6db0ade