Shoemaker D D, Legha S S, Cysyk R L
Pharmacology. 1978;16(4):221-5. doi: 10.1159/000136771.
The acridine derivative 4'-(9-acridinylamino)-methanesulfon-m-anisidide (AMSA, NSC-141549), a new antitumor agent undergoing phase I clinical evaluation, is highly active against B16 melanoma in vivo. AMSA was found to be concentrated in B16 melanoma cells in vivo and remained at high concentrations for at least 72 h. Subcellular fractionation of B16 melanoma cells revealed the drug to be bound to melanin granules. The results suggest the possible use of AMSA in human melanoma and the design of other antimelanoma agents that would exploit the affinity of the acridine nucleus for melanin.
吖啶衍生物4'-(9-吖啶基氨基)-甲磺酰间茴香胺（AMSA，NSC-141549）是一种正在进行I期临床评估的新型抗肿瘤药物，在体内对B16黑色素瘤具有高度活性。研究发现，AMSA在体内可在B16黑色素瘤细胞中富集，并在至少72小时内保持高浓度。对B16黑色素瘤细胞进行亚细胞分级分离显示，该药物与黑色素颗粒结合。这些结果表明AMSA可能用于治疗人类黑色素瘤，并为设计其他利用吖啶核与黑色素亲和力的抗黑色素瘤药物提供了思路。
