Synthesis and Antitumor Activities of Novel Benzoylphenylurea Derivatives.
作者:Hiroshi OKADA、Tohru KOYANAGI、Nobutoshi YAMDA、Takahiro HAGA
DOI:10.1248/cpb.39.2308
日期:——
Seventy novel benzoylphenylurea compounds were synthesized and their antitumor activities were examined in vivo against P388 leukemia. N-(2-Nitrobenzoyl)-N'-[4-(2-pyrimidinyloxy)phenyl]ureas showed the highest antitumor activities when dosed intraperitoneally or orally. Their structure-activity relationships were examined with particular focus on the position and the variety of subsitituent on each aryl ring.
合成了七十种新的苯甲酰苯基脲化合物,并对其在体内对P388白血病的抗肿瘤活性进行了研究。N-(2-硝基苯甲酰)-N'-[4-(2-吡啶基氧)苯基]脲在腹腔注射或口服给药时显示出最高的抗肿瘤活性。研究了它们的结构-活性关系,特别关注每个芳环上取代基的位置和种类。