SYNKAVIT AND ITS DIRECT LABELING WITH I-125, AS A POTENTIAL ANTICANCER DRUG

The compound known as ''synkavit'' is a diphosphate derivative of vita min K, (menadion), which is capable of being selectively accumulated i n certain tumour cells, and covalently bonded to DNA producing conside rable DNA damage. On the other hand, iodine-125 nuclide incorporated i nto the nucleus of living cells causes extreme radiotoxic effects. Con sequently, synkavit can be used as a specific carrier of iodine-125 in to the nucleus of tumour cells. Thus, its iodo-derivatives have become interesting agents on the potential application of iodine-125 in canc er therapy. 6-Iodo-synkavit is a unique iodo-derivative described in t he literature. In addition, its synthesis and radioiodination is still problematic, and consequently the results obtained using 6-iodo-synka vit labelled with iodine-125 remains in question. For this reason, the synthesis of 6-iodo-synkavit was examined in this study. It is finall y determined that a mixture of different iodo-isomers of synkavit has been produced rather than its specific 6-iodo-isomer, when the synthet ic sequence was begun with the direct sulfonation of 2-methyl-naphthal ene. On the other hand, it is also determined that synkavit can direct ly be radioiodinated using different iodination techniques, and iodoge n especially can be successfully used as an oxidative agent.