Stermitz F R, Gillespie J P, Amoros L G, Romero R, Stermitz T A, Larson K A, Earl S, Ogg J E
J Med Chem. 1975 Jul;18(7):708-13. doi: 10.1021/jm00241a014.
A facil synthesis of benzophenanthridinium salts has been developed and used for preparing a number of these compounds. The antitumor activities in mouse leukemia L1210 (LE) and P388 (PS) were determined as well as some selected antimicrobial activities. Although antitumor activity was exhibited by several of the derivatives, none was as active as the naturally occurring alkaloid fagaronine. Fagaronine was made available as a synthetic by an improved procedure. Some structure-activity relationships among antitumor benzophenanthridinium salts are discussed.
已开发出一种简便的苯并菲啶盐合成方法，并用于制备多种此类化合物。测定了其对小鼠白血病L1210（LE）和P388（PS）的抗肿瘤活性以及一些选定的抗菌活性。尽管几种衍生物都表现出抗肿瘤活性，但没有一种像天然存在的生物碱法格龙宁那样活跃。通过改进的方法可以通过合成获得法格龙宁。讨论了抗肿瘤苯并菲啶盐之间的一些构效关系。
