Vitamin D Analogue: Potent Antiproliferative Effects on Cancer Cell Lines and Lack of Hypercalcemic Activity

Autor: Alejandro Carlos Curino, Norberto Ariel Gandini, Maria Marta Facchinetti, Yagamare Fall, Marcos L. Rivadulla, Generosa Gómez, Alejandro López Romero, María Eugenia Fermento, María Julia Ferronato, Débora Gisele Salomón, Manuel Pérez, Xenxo Pérez-García
Rok vydání: 2015
Předmět:
Zdroj: Archiv der Pharmazie. 348:315-329
ISSN: 0365-6233
Popis: The active form of vitamin D3, 1α,25(OH)2D3, plays a major role in maintaining calcium/phosphate homeostasis. In addition, it is a potent antiproliferative and pro-differentiating agent. Unfortunately, it usually causes hypercalcemia in vivo when effective antitumour doses are used. It has therefore been found necessary to synthesise new analogues that retain or even increase the antitumour effects but preclude hypercalcemia. This report presents the synthesis of a novel Gemini vitamin D analogue (UVB1) and its biological evaluation. We demonstrate that this compound has potent antitumoural effects over a wide panel of tumour cell lines while showing lack of hypercalcemic activity and toxicity effects in in vivo assays.
Databáze: OpenAIRE