DiStefano V, Evans I, Myers-Robfogel M, Estes J, Godleski S A
J Natl Cancer Inst. 1983 Dec;71(6):1289-93.
Two phenylthioalkylamines, phenylthioethylamine (PTEA) and phenylthiopropylamine (PTPA), were prepared and tested for cytotoxicity in vitro and as antitumor agents in (C57BL X DBA/2)F1 (BDF1) mice. Low concentrations of PTEA (median effective concentrations of 8.0, 12.0, and 1.3 micrograms PTEA/ml) inhibited the growth of P388 murine lymphoma, L1210 leukemia, and B16 melanoma cells in culture. PTPA was more effective; concentrations of 0.80, 0.56, and 0.35 micrograms PTPA/ml inhibited the growth of P388, L1210, and B16 in vitro by 50%. PTEA and PTPA treatment increased survival times in BDF1 mice bearing the P388 lymphoma, L1210 leukemia, B16 melanoma, and Lewis lung tumors. Multiple daily administrations of the test compounds were more effective than single daily injections in increasing the life-span in mice bearing the P388 lymphoma and B16 melanoma. Both PTEA and PTPA inhibited the enzyme copper-zinc superoxide dismutase.
制备了两种苯硫基烷基胺，苯硫基乙胺（PTEA）和苯硫基丙胺（PTPA），并对其进行体外细胞毒性测试以及作为抗肿瘤剂在（C57BL×DBA/2）F1（BDF1）小鼠体内进行测试。低浓度的PTEA（中位有效浓度分别为8.0、12.0和1.3微克PTEA/毫升）在培养中抑制了P388鼠淋巴瘤、L1210白血病和B16黑色素瘤细胞的生长。PTPA更有效；0.80、0.56和0.35微克PTPA/毫升的浓度在体外使P388、L1210和B16的生长受到50%的抑制。PTEA和PTPA处理延长了携带P388淋巴瘤、L1210白血病、B16黑色素瘤和Lewis肺癌的BDF1小鼠的存活时间。在延长携带P388淋巴瘤和B16黑色素瘤小鼠的寿命方面，每日多次给药比每日单次注射更有效。PTEA和PTPA均抑制了铜锌超氧化物歧化酶。
