Premium
Improved synthesis on solid phase of dithiocarbamic cRGD ‐derivative and 99m Tc ‐radiolabelling
Author(s) -
Caporale Andrea,
Bolzati Cristina,
Incisivo Giuseppina Maria,
Salvarese Nicola,
Grieco Paolo,
Ruvo Menotti
Publication year - 2019
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.3140
Subject(s) - chemistry , angiogenesis , solid phase synthesis , dithiocarbamate , combinatorial chemistry , stereochemistry , biochemistry , peptide , cancer research , organic chemistry , medicine
In the field of angiogenesis, small cyclic pentapeptides containing the RGD motif are playing a relevant role for their high affinity and specificity for integrin receptors and for the possibility to act at both therapeutic and diagnostic level by inhibiting pathological angiogenesis and by serving as shuttles to deliver imaging‐probe including SPECT/PET radionuclides to specific tissues. In the last decade, several new protocols were reported in literature for the direct synthesis of cyclic RDG either in solution or by SPPS. Here, we have elaborated and tested some alternative approaches using different resins and different protective groups. The introduction of the dithiocarbamate function, useful to complex radio‐metals suitable for nuclear medicine applications, has also been considered and achieved.