Ejima A, Terasawa H, Sugimori M, Ohsuki S, Matsumoto K, Kawato Y, Yasuoka M, Tagawa H
Exploratory Research Laboratories I, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
Chem Pharm Bull (Tokyo). 1992 Mar;40(3):683-8. doi: 10.1248/cpb.40.683.
Several E-ring-modified analogues of (RS)-camptothecin were synthesized by total synthesis via Friedländer condensation and evaluated for cytotoxicity and antitumor activity against P388 mouse leukemia cells. Among them, (RS)-20-deoxyamino-7-ethyl-10-methoxycamptothecin (25c) was found to be more active than (RS)-camptothecin (1) in the in vivo assay.
通过Friedländer缩合全合成法合成了几种（RS）-喜树碱的E环修饰类似物，并对其针对P388小鼠白血病细胞的细胞毒性和抗肿瘤活性进行了评估。其中，（RS）-20-脱氧氨基-7-乙基-10-甲氧基喜树碱（25c）在体内试验中被发现比（RS）-喜树碱（1）更具活性。
