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Contraceptive activity of a spermicidal aryl phosphate derivative of bromo-methoxy- zidovudine (compound WHI-07) in rabbits Osmond J. D’Cruz, Ph.D., Fatih M. Uckun, M.D., Ph.D. Fertility and Sterility Volume 79, Issue 4, Pages (April 2003) DOI: /S (02)
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FIGURE 1 Chemical structure of WHI-07 (5-bromo-6-methoxy-5,6-dihydro-3′-azidothymidine-5′-[p-bromophenyl] methoxyalaninyl phosphate). WHI-07 (molecular weight, ) differs from AZT by the presence of 5-bromo and 6-methoxy groups on the thymine ring, a phenyl phosphate group with an alanine side chain, and a bromo substituent on the C-5 position of the phenyl ring. D’Cruz. Contraceptive activity of WHI-07.Fertil Steril 2003. Fertility and Sterility , DOI: ( /S (02) )
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FIGURE 2 (A), Concentration-dependent inhibition of rabbit sperm motility in rabbit semen by WHI-07. Fresh, pooled semen aliquots were suspended in serial twofold drug concentrations ranging from 0.97 to 125 μM (final concentration) or vehicle (0.12% DMSO), and the percentage of motile sperm were evaluated by CASA. Results are expressed as mean values. (B), Time-dependent sperm immobilization by WHI-07. Fresh, pooled semen aliquots were incubated with 0.2% DMSO alone or 200 μM WHI-07 in 0.2% DMSO, and the percentage of motile sperm were evaluated by CASA at timed intervals of 15, 30, 45, 60, and 75 minutes. Results are expressed as mean values. D’Cruz. Contraceptive activity of WHI-07.Fertil Steril 2003. Fertility and Sterility , DOI: ( /S (02) )
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