Okada H, Koyanagi T, Yamada N, Haga T
Central Research Institute, Ishihara Sangyo Kaisha, Ltd., Shiga, Japan.
Chem Pharm Bull (Tokyo). 1991 Sep;39(9):2308-15. doi: 10.1248/cpb.39.2308.
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 substituent on each aryl ring.
合成了70种新型苯甲酰基苯基脲化合物，并在体内检测了它们对P388白血病的抗肿瘤活性。当通过腹腔注射或口服给药时，N-（2-硝基苯甲酰基）-N'-[4-（2-嘧啶基氧基）苯基]脲显示出最高的抗肿瘤活性。特别关注每个芳环上取代基的位置和种类，研究了它们的构效关系。
