Various kinds of water-soluble 9-acyloxyellipticine derivatives were synthesized in a search for compounds with potent antitumor activity. Antitumor activities against several tumors in mice (P388 leukemia, colon 26, Lewis lung carcinoma and B16 melanoma) were evaluated by using intravenous administration. Many compounds exhibited good antitumor activities; in particular, the glutarate derivative (5o) showed potent antitumor activity. This comopound (5o) may be converted to 9-hydroxyellipticine (2) by enzyme-catalyzed hydrolysis in the body.
合成了多种
水溶性9-酰氧基椭圆碱衍
生物,以寻找具有强抗肿瘤活性的化合物。通过静脉给药评估了对小鼠几种肿瘤(P388白血病、结肠26、刘易斯肺癌和B16
黑色素瘤)的抗肿瘤活性。许多化合物表现出良好的抗肿瘤活性;特别是
戊二酸衍
生物(5o)显示出强的抗肿瘤活性。该化合物(5o)可能通过体内酶催化的
水解转化为9-羟基椭圆碱(2)。