摘要
目的 寻找高效低毒的抗肿瘤药物。方法和结果 本文设计并合成了新的C4 位 β构型的酯取代的衍生物 38个 (II 1～II 38) ,并进行了体外对L12 10 细胞和KB细胞的抗肿瘤活性实验。结论 脂肪酯的活性强于芳香酯 ,其中以II 10的活性最强 ,超过etoposide 2个数量级。脂肪酯中主链不超过 3个碳原子的活性较好。在芳香酯中 ,苯环上连接吸电子基的化合物的活性稍强于连接有供电子基的化合物。
AIM To search for more potential and lower toxicity antitumor drugs. METHODS AND RESULTS Thirty eight new 4 β ester substituted 4 deoxy 4′ demethylepipodophylotoxin derivatives(II 1～II 38) were designed and synthesized. All compounds were screened in vitro against L 1210 leukemia and KB cells. CONCLUSION Fatty esters showed higher activity than aromatic esters. II 10 exhibited the highest activity, which is more than 100 fold of etoposide. For fatty esters, the compounds with less than 3 carbons in the main chain have higher activity, while for aromatic esters, those having electron attracting substituents in the aromatic ring are more active.
出处
《药学学报》
CAS
CSCD
北大核心
2000年第5期353-357,共5页
Acta Pharmaceutica Sinica
