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Design and synthesis of new imidazo[1,2- a ]pyridine and imidazo[1,2- a ]pyrazine derivatives with antiproliferative activity against melanoma cells
- Source :
- European Journal of Medicinal Chemistry. 108:623-643
- Publication Year :
- 2016
- Publisher :
- Elsevier BV, 2016.
-
Abstract
- Melanoma is an aggressive form of skin cancer and it is generally associated with poor prognosis in patients with late-stage disease. Due to the increasing occurrence of melanoma, there is a need for the development of novel therapies. A new series of diarylamide and diarylurea derivatives containing imidazo[1,2-a]pyridine or imidazo[1,2-a]pyrazine scaffold was designed and synthesized to investigate their in vitro efficacy against the A375P human melanoma cell line. We found several compounds expressing submicromolar IC50 values against the A375P cells, from which 15d, 17e, 18c, 18h, 18i demonstrated the highest potencies with IC50 below 0.06 μM.
- Subjects :
- Pyrazine
Pyridines
Antineoplastic Agents
01 natural sciences
Structure-Activity Relationship
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Cell Line, Tumor
Drug Discovery
Pyridine
medicine
Humans
In patient
Melanoma
IC50
Cell Proliferation
Pharmacology
Dose-Response Relationship, Drug
Molecular Structure
010405 organic chemistry
Organic Chemistry
Imidazoles
General Medicine
medicine.disease
0104 chemical sciences
chemistry
Cell culture
Drug Design
Pyrazines
030220 oncology & carcinogenesis
Cancer research
Human melanoma
Drug Screening Assays, Antitumor
Skin cancer
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 108
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....bde15e26b148e3cf59bc8cb5ff4d7712
- Full Text :
- https://doi.org/10.1016/j.ejmech.2015.12.001