Bonjouklian R, Phillips M L, Kuhler K M, Grindey G B, Poore G A, Schultz R M, Altom M G
J Med Chem. 1986 Dec;29(12):2472-7. doi: 10.1021/jm00162a009.
Analogues of the synthetic antitumor phospholipid ALP (1-octadecyl-2-methyl-sn-glycero-3-phosphocholine; alkyl lysophospholipid) in which the 1-ether oxygen atom has been removed have been prepared and evaluated for in vitro and in vivo anticancer activity. Compounds are presented in which the saturated long chain varies in length from 8 to 25 carbon atoms. Sites of unsaturation are also incorporated into the framework in some examples. In particular, rac-(2-ethoxyeicosyl)phosphocholine (10) displays the best in vivo activity of the chemical series against a variety of transplanted tumors and activates murine peritoneal macrophages to express tumor cytotoxicity in vitro. However, 10 does not offer the wide spectrum of antitumor activity we feel necessary to warrant further study.
已制备出1-醚氧原子被去除的合成抗肿瘤磷脂ALP（1-十八烷基-2-甲基-sn-甘油-3-磷酸胆碱；烷基溶血磷脂）类似物，并对其体外和体内抗癌活性进行了评估。展示了饱和长链长度在8至25个碳原子之间变化的化合物。在一些实例中，不饱和位点也被纳入骨架中。特别地，消旋-(2-乙氧基二十烷基)磷酸胆碱（10）在该化学系列中对多种移植肿瘤表现出最佳的体内活性，并在体外激活小鼠腹腔巨噬细胞以表达肿瘤细胞毒性。然而，10并未提供我们认为有必要进行进一步研究所需的广泛抗肿瘤活性谱。
