Affinity therapeutics. 1. Selective incorporation of 2-thiouracil derivatives in murine melanomas. Cytostatic activity of 2-thiouracil arotinoids, 2-thiouracil retinoids, arotinoids, and retinoids.
The incorporation of 2-[35S]thiouracil and two of its derivatives into murine melanomas, in vivo, was studied. It was confirmed [J. R. Whittaker, J. Biol. Chem., 246, 6217--6226 (1971)] that 2-thiouracil has a marked affinity for melanin-producing tissue and that an affinity for such tissue could be sustained by 5-substituted 2-thiouracils. A series of derivatives of arotinoids and retinoids, with or without a 2-thiouracil group as a potential carrier to obtain affinity for melanomas, was examined for cytostatic activity, in vitro. None of these showed significant activity against murine melanomas.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism; D002478:Cells, Cultured; D055598:Chemical Phenomena; D002621:Chemistry; D008545:Melanoma / Q000378:metabolism*; D051379:Mice; D008811:Mice, Inbred DBA; D009374:Neoplasms, Experimental / Q000378:metabolism; D013889:Thiouracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism; D014018:Tissue Distribution; D014212:Tretinoin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000378:metabolism
D000970:Antineoplastic Agents; D014212:Tretinoin; D013889:Thiouracil