876938-99-7Relevant articles and documents
Synthesis and biological evaluation of 9-(5′,5′-difluoro- 5′-phosphonopentyl)guanine derivatives for PNP-inhibitors
Hikishima, Sadao,Isobe, MacHiko,Koyanagi, Satoru,Soeda, Shinji,Shimeno, Hiroshi,Shibuya, Shiroshi,Yokomatsu, Tsutomu
, p. 1660 - 1670 (2007/10/03)
9-(5′,5′-Difluoro-5′-phosphonopentyl)guanine (DFPP-G) and its hypoxanthine analogue (DFPP-H) were modified by introducing a methyl group to all possible positions of the linker connecting a purine and difluoromethylenephosphonic acid moiety to evaluate the effects of the methyl group on inhibition against purine nucleoside phosphorylase. The methyl group on the linker affected the inhibition in a positional-dependent manner. Inhibitory potency of α-methyl and β-methyl-substituted analogues of DFPP-H increased by about 600- to 1000-fold upon converting to cyclopropane nucleotide analogue (±)-4.