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  • Title: Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells.
    Author: Garamvölgyi R, Dobos J, Sipos A, Boros S, Illyés E, Baska F, Kékesi L, Szabadkai I, Szántai-Kis C, Kéri G, Őrfi L.
    Journal: Eur J Med Chem; 2016 Jan 27; 108():623-643. PubMed ID: 26724730.
    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.
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