University of Cape Town

The South African Nuclear Energy Corporation Limited

Mohamed Iqbal Parker

Roger Hunter

Jan Rijn Zeevaart

Cathryn Helena Stanford Driver

Catherine Hart Kaschula

This invention relates new radiopharmaceutical conjugates for use in improved methods of diagnosis and treatment of cancer. The radiopharmaceutical conjugate comprises, in sequence: a metabolite that targets tumour cells, bound to a chelating agent capable of containing a radionuclide, bound to a linker capable of binding with an EPR agent in vitro or in vivo; or a chelating agent capable of containing a radionuclide, bound to a metabolite that targets tumour cells, bound to a linker capable of binding with an EPR agent in vitro or in vivo. The radiopharmaceutical conjugates of the present invention provide active and passive targeted radio nuclide delivery systems that can help to improve the biodistribution and pharmacological toxicity of the radiopharmaceuticals used for the diagnosis and therapy of cancer.

Radiopharmaceutical conjugate of a metabolite and an EPR agent, for targeting tumour cells

Organosulfur compounds of the general formula (2) are described, wherein Rand Rare linear or branched C1-C5 alkyl; linear or branched C1-C5 alkenyl with the proviso that Ris not prop-1-enyl (allyl); substituted linear or branched C1-C5 alkenyl or substituted linear or branched C1-C5 alkyl, in which the substituents are selected from OR, NRR, COOR, CON&#x2014;RR, in which Ris selected from H, COR, para-methoxybenzyl and trialkylsilyl, in which Ris alkyl or substituted alkyl; RN and Rare alkyl or Rand Rtogether form a phthalimido group; Ris alkyl or substituted alkyl; and Rand Rare alkyl or substituted alkyl; substituted or unsubstituted aromatic specifically where Rand Rare benzyl, para-methoxybenzyl and/or ortho,para-methoxybenzyl and substituted or unsubstituted heteroaromatic. The compounds can be used for inhibiting the growth of tumor cells and for treating cancer. A pharmaceutical composition and a method of preparing the compounds are also described. 

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Cape Town, South Africa

Mohamed Iqbal Parker