Journal
ANTI-CANCER DRUGS
Volume 19, Issue 8, Pages 789-792Publisher
LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/CAD.0b013e32830ce4d8
Keywords
antitumor agents; in-vitro anti proliferative activities; kinase inhibitory activities; meridianins
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Funding
- European Union Prokinase Research Consortium
- PAC (Plan Auvergne Cancer)/CLARA (Canceropole Lyon Auvergne Rhone-Alpes)
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Marine alkaloid meridianin G derivatives, substituted on the pyrimidine ring by aryl groups, were evaluated for their kinase inhibitory potencies and their in-vitro antiproliferative activities. The derivatives were tested toward a panel of nine protein kinases (KDR, IGF-1R, c-Met, RET, c-Src, c-Abl, PKA, CDK2/cyclin A, and HER-1) and their in-vitro anti proliferative activities were evaluated toward a human fibroblast primary culture and two human solid cancer cell lines (MCF-7 and PA 1). Despite weak kinase inhibitory potencies, high in-vitro antiproliferative activities were found for compounds 5, 7,12, and 14, which do not interfere with the PA 1 cell cycle and may be considered as direct cytolysis or apoptosis inducers.
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