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新型双腙桥联4-去甲氧基柔红霉素衍生物SC33428对小鼠实验性肿瘤的活性

Activity of SC33428, a novel bishydrazone-bridged derivative of 4-demethoxydaunorubicin, against experimental tumors in mice.

作者信息

Dawson K M

出版信息

Cancer Res. 1983 Jun;43(6):2880-3.

PMID:6573953
Abstract

SC33428, a novel bishydrazone-bridged analogue of 4-demethoxydaunorubicin, has been tested for antitumor activity in a range of experimental mouse tumor systems and has been found to be active when administered i.p., i.v., or p.o. When compared to Adriamycin, SC33428 was 4 times more potent and had antitumor activity which was superior against i.p. or i.v. L1210 leukemia, similar against i.p. P388 leukemia and i.v. Lewis lung carcinoma, and inferior against i.p. B16 melanoma. When compared to 4-demethoxydaunorubicin, SC33428 was 4 times less potent but a much more effective antitumor agent when given i.p. against i.p. L1210, P388, and B16 tumors. However, when given i.v. or p.o., the two compounds had similar potency and efficacy against systemic P388 and L1210 leukemias.

摘要

SC33428是一种新型的双腙桥连的4-去甲氧基柔红霉素类似物,已在一系列实验小鼠肿瘤模型中测试了其抗肿瘤活性,结果发现腹腔注射、静脉注射或口服给药时均具有活性。与阿霉素相比,SC33428的效力高4倍,对腹腔注射或静脉注射的L1210白血病的抗肿瘤活性更强,对腹腔注射的P388白血病和静脉注射的Lewis肺癌的抗肿瘤活性相似,而对腹腔注射的B16黑色素瘤的抗肿瘤活性较弱。与4-去甲氧基柔红霉素相比,SC33428的效力低4倍,但腹腔注射给药时对腹腔注射的L1210、P388和B16肿瘤是一种更有效的抗肿瘤药物。然而,静脉注射或口服给药时,这两种化合物对全身性P388和L1210白血病的效力和疗效相似。

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