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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

Authors :
Anna Sipos
Rita Garamvölgyi
Ferenc Baska
László Kékesi
László Őrfi
Csaba Szántai-Kis
Judit Dobos
Sándor Boros
Eszter Illyés
György Kéri
István Szabadkai
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.

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