期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 21, 页码 6800-6807出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm801003y
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资金
- Ministero dell' Universita e della Ricerca Scientifica e Tecnologica [PRIN 2006]
A small series of aminobisphosphonates (N-BPs) structurally related to zoledronic acid was synthesized with the aim of improving activity toward activation of human gamma delta T cells and in turn their in vivo antitumor activity. The absence of the 1-OH moiety, together with the position and the different basicity of the nitrogen, appears crucial for antitumor activity. In comparison to zoledronic acid, compound 6a shows a greater ability to activate gamma delta T cells expression (100 times more) and a proapoptotic effect that is better than zoledronic acid. The potent activation of gamma delta T cells, in addition to evidence of the in vivo antitumor activity of 6a, suggests it may be a new potential drug candidate for cancer treatment.
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