title: Synthesis and biological evaluation of 90Y-labeled porphyrin-DOTA conjugate: a potential molecule for targeted tumor therapy.
abstract: An unsymmetrically substituted porphyrin, 5-[4-(3-amino)-n-propyloxyphenyl]-10,15,20-tris-(4-carboxymethyleneoxyphenyl)porphyrin, was synthesized and coupled with p-NCS-benzyl-DOTA [p-isothiocyanato-benzyl-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid] for exploring its possible potential in targeted tumor therapy. The porphyrin-DOTA conjugate was radiolabeled with 90Y, obtained from a 90Sr/90Y electrochemical generator, developed in-house. Biodistribution studies performed in Swiss mice bearing fibrosarcoma tumor showed good tumor uptake (∼3.4% injected activity in per g of tumor) within 30 minutes postinjection. The tumor activity decreased with the progress of time, however, tumor to blood and tumor to muscle ratios considerably increased at 4 days postadministration owing to the clearance of the initially accumulated activities from the nontarget organs. The nonaccumulated activity exhibited major clearance through renal pathway.
authors.affiliation: 1 Radiopharmaceuticals Division, Bhabha Atomic Research Centre , Trombay, Mumbai, India .
authors.forename: Sweety
authors.initials: S
authors.lastname: Mittal
authors.forename: Mohini
authors.initials: M
authors.lastname: Bhadwal
authors.forename: Tapas
authors.initials: T
authors.lastname: Das
authors.forename: Haladhar Dev
authors.initials: HD
authors.lastname: Sarma
authors.forename: Rubel
authors.initials: R
authors.lastname: Chakravarty
authors.forename: Ashutosh
authors.initials: A
authors.lastname: Dash
authors.forename: Sharmila
authors.initials: S
authors.lastname: Banerjee
authors.forename: M R A
authors.initials: MR
authors.lastname: Pillai
mesh_terms: D000818:Animals; D005260:Female; D005354:Fibrosarcoma / Q000532:radiotherapy; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry*; D007668:Kidney / Q000528:radiation effects; D051379:Mice; D011166:Porphyrins / Q000138:chemical synthesis* / Q000737:chemistry*; D011868:Radioisotopes / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000627:therapeutic use*; D011878:Radiotherapy; D017550:Spectroscopy, Fourier Transform Infrared; D013326:Strontium Radioisotopes / Q000737:chemistry; D013997:Time Factors; D014018:Tissue Distribution; D015021:Yttrium Radioisotopes / Q000737:chemistry*
chemical_list: D006573:Heterocyclic Compounds, 1-Ring; D011166:Porphyrins; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D013326:Strontium Radioisotopes; D015021:Yttrium Radioisotopes; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid