Synthesis and evaluation of 2-(p-isothiocyanatobenzyl)-trans-cyclohexyl-DTPA linked to antibody B72.3 for radioimmunoimaging and therapy
- 1. National Institutes of Health, Bethesda, MD (USA)
Description
Radioimmunotherapy with the α-emitter Bi-212 chelate linked to antibody is of current interest in oncology. Isothiocyanatobenzyl cyclohexyl-DTPA (CHX-DPTA) was synthesized to incorporate the semi-rigid geometry conferred by the cyclohexyl ring and thereby increase metal complex stability in vivo for therapeutic radionuclides. BOC-p-nitrophenylalanine was converted to the amide of trans-1,2-diaminocyclohexane. After deprotection, the amide was reduced, and the resulting triamine alkylated to the pentaacetic acid. Two pairs of diastereomers were isolated and characterized. Biodistribution results indicate that inclusion of the cyclohexyl structure into a DTPA resulted in an acyclic ligand useful for radioimmunotherapy with either Y-90 or Bi-212
Additional details
Publishing Information
- Publisher
- American Chemical Society.
- Imprint Place
- Washington, DC (USA)
- Imprint Title
- American Chemical Society, Division of Inorganic Chemistry, Inc.
- Imprint Pagination
- 158 p.
- Journal Page Range
- p. 22-23.
Conference
- Title
- 200. American Chemical Society national meeting.
- Dates
- 26-31 Aug 1990.
- Place
- Washington, DC (USA).
INIS
- Country of Publication
- United States
- Country of Input or Organization
- United States
- INIS RN
- 22022940
- Subject category
- S62: RADIOLOGY AND NUCLEAR MEDICINE; S62: RADIOLOGY AND NUCLEAR MEDICINE; S38: RADIATION CHEMISTRY, RADIOCHEMISTRY AND NUCLEAR CHEMISTRY;
- Resource subtype / Literary indicator
- Conference
- Descriptors DEI
- BISMUTH COMPLEXES; BISMUTH 212; CHEMICAL PREPARATION; DTPA; IMMUNOGLOBULINS; IMMUNOTHERAPY; LABELLING; RADIOIMMUNODETECTION; RADIOPHARMACEUTICALS; RADIOTHERAPY; YTTRIUM 90
- Descriptors DEC
- ALPHA DECAY RADIOISOTOPES; AMINO ACIDS; BETA DECAY RADIOISOTOPES; BETA-MINUS DECAY RADIOISOTOPES; BISMUTH ISOTOPES; CARBOXYLIC ACIDS; CHELATING AGENTS; COMPLEXES; DAYS LIVING RADIOISOTOPES; DIAGNOSTIC TECHNIQUES; DRUGS; GLOBULINS; HEAVY NUCLEI; HOURS LIVING RADIOISOTOPES; INTERMEDIATE MASS NUCLEI; ISOMERIC TRANSITION ISOTOPES; ISOTOPE APPLICATIONS; ISOTOPES; LABELLED COMPOUNDS; MATERIALS; MEDICINE; MINUTES LIVING RADIOISOTOPES; NUCLEI; ODD-ODD NUCLEI; ORGANIC ACIDS; ORGANIC COMPOUNDS; PROTEINS; RADIOACTIVE MATERIALS; RADIOISOTOPES; RADIOPROTECTIVE SUBSTANCES; RESPONSE MODIFYING FACTORS; SYNTHESIS; THERAPY; TRACER TECHNIQUES; YTTRIUM ISOTOPES
Optional Information
- Notes
- Paper INOR 73.
- Secondary number(s)
- CONF-900802--.