Cookies on this website
We use cookies to ensure that we give you the best experience on our website. If you click 'Continue' we'll assume that you are happy to receive all cookies and you won't see this message again. Click 'Find out more' for information on how to change your cookie settings.

A small series of aminobisphosphonates (N-BPs) structurally related to zoledronic acid was synthesized with the aim of improving activity toward activation of human gammadelta 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 gammadelta T cells expression (100 times more) and a proapoptotic effect that is better than zoledronic acid. The potent activation of gammadelta 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.

Original publication

DOI

10.1021/jm801003y

Type

Journal article

Journal

J med chem

Publication Date

13/11/2008

Volume

51

Pages

6800 - 6807

Keywords

Amines, Animals, Antineoplastic Agents, Apoptosis, Cell Line, Tumor, Diphosphonates, Drug Design, Humans, Lymphocyte Activation, Mice, Mice, SCID, Molecular Structure, Receptors, Antigen, T-Cell, gamma-delta, Structure-Activity Relationship