Wätjen F, Buchardt O, Langvad E
J Med Chem. 1982 Aug;25(8):956-60. doi: 10.1021/jm00350a014.
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.
研究了2-[³⁵S]硫尿嘧啶及其两种衍生物在体内掺入小鼠黑色素瘤的情况。已证实[J. R. 惠特克，《生物化学杂志》，246, 6217 - 6226(1971)]，2-硫尿嘧啶对产生黑色素的组织有显著亲和力，并且5-取代的2-硫尿嘧啶可以维持对这种组织的亲和力。研究了一系列有或没有2-硫尿嘧啶基团作为潜在载体以获得对黑色素瘤亲和力的类视黄醛和类维生素A衍生物的体外细胞抑制活性。这些衍生物均未显示出对小鼠黑色素瘤的显著活性。
