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Methylenebisphosphonate and its monofluoro-, difluoro- and dichloro- derivatives inhibited growth of amoebae of Dictyostelium discoideum. Dichloromethylenebisphosphonate was the most potent inhibitor of amoebal growth whereas difluoromethylenebisphosphonate was the least potent inhibitor. Each of the bisphosphonates was taken up by the amoebae and incorporated into the corresponding beta, gamma-methylene analogue of adenosine triphosphate. Two of the bisphosphonates were also incorporated into the corresponding analogues of diadenosyl tetraphosphate. No correlation was found between the ability of the bisphosphonates to inhibit amoebal growth and the extent to which they were metabolised.

Original publication

DOI

10.1016/0006-291x(92)91574-a

Type

Journal article

Journal

Biochem biophys res commun

Publication Date

30/11/1992

Volume

189

Pages

414 - 423

Keywords

Adenosine Triphosphate, Animals, Biological Transport, Dictyostelium, Diphosphates, Diphosphonates, Kinetics, Magnetic Resonance Spectroscopy, Structure-Activity Relationship