5-(2-methylene estrone 3-methyl ether)-3,3,10,10-tetramethyl-1,2-dithia-5,8-diazabicyclodecane

Description

Dads-E can be used in use of diaminodithiol for labeling small molecules with technetium-99m.The estrone derivative was prepared by alkylation of DADS while the fatty acid derivative -N,N'-bisethylenediamine hydrochloride, DADT-FA) was synthesized by alkylation of DADS followed by reduction. DADS-E was labeled in ethanol at elevated temperatures while DADT-FA was labeled at room temperature, both by stannous reduction. Paper chromatography showed both to be labeled and reverse-phase HPLC showed multiple peaks for both. Serum stability studies were performed by incubation at 37 degrees C with aliquots removed at 1 min and 1 day for analysis by size-exclusion HPLC. Initially, little pertechnetate or binding to serum proteins was observed whereas after 1 day the majority of activity in both cases was protein bound with 20 and 38% pertechnetate appearing for DADT-FA and DADS-E respectively.