Radioactive cyclopentadienyl complexes of rhenium - for labelling proteins e.g. polyclonal or monoclonal antibodies or for targetted radiotherapy esp. of tumours

摘要

Radioactive cyclopentadienyl rhenium complexes of formula (I) are new. In (I) R1 and R2 = any substit. provided R1 and R2 are not both H; R2 = pref. H; Re = a radioactive rhenium isotope. Specifically substit. can be aliphatic chains, aromatic, hydroaromatic or heterocyclic gps.. USE/ADVANTAGE - (I) in which R1 = cOOH and R2 = COOH or H can be used either directly or in the form of an activated carboxylic acid deriv. for labelling proteins, esp. polyclonal or monoclonal antibodies. (I) can also be used in radiotherapy esp. of tumours. Depending on the choice of R substd. (I) can be tailored for the treatment of various tumours e.g. Re-186 cyrherenyl ethylnyl oestradiol enriches in tissues contg. oestrogen receptors and can therefore be used for the targetted radiotherapy of mammory tumour and the corresp. metastases. Previous rhenium complexes have only had very reduced possibilities for chemical variation, unlike (I) where many variations are possible. The rhenium complexes (I) are analagous to cymantrene and are hence called cyrhetrene.