title: Synthesis and selective tumor targeting properties of water soluble porphyrin-Pt(II) conjugates.
abstract: We have designed and synthesized a series of novel water soluble porphyrins and their platinum(II) conjugates, cis-[(Por)Pt(dmso)X], where Por=5-(4-pyridyl)-10,15,20-tris(4-sulfonatophenyl)porphyrin) (PyTPPS) or 5-[4-(3-aminopropyl)pyridiniumyl]-10,15,20-tris(4-sulphonatophenyl)porphyrin (PyTPPS-NPn), X=2Cl, 1,1-cyclobutanedicarboxylic acid, oxalate, or malonate. Their biodistribution in tumor bearing mouse was examined along with their antitumor activity against murine leukemia L1210 cell line. The representative complex 1 exhibited a significant accumulation in tumor tissue with a tumor/muscle ratio of 7 after 24 h post injection. The antitumor activity of the title compounds was marginal (T/C: 95-117%), but it was found that platinum(II) coordination to the porphyrin periphery did not affect the tumor accumulating properties of the porphyrin permitting further derivatization for efficient delivery of the Pt(II) antitumor agent.
authors.affiliation: Korea Institute of Science and Technology, 130-650, Seoul, South Korea.
authors.forename: Rita
authors.initials: R
authors.lastname: Song
authors.forename: Yeong Sang
authors.initials: YS
authors.lastname: Kim
authors.forename: Youn Soo
authors.initials: YS
authors.lastname: Sohn
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D051379:Mice; D009368:Neoplasm Transplantation; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D009928:Organ Specificity; D010984:Platinum / Q000737:chemistry*; D011166:Porphyrins / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D013379:Substrate Specificity; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D011166:Porphyrins; D010984:Platinum