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FCE 23762（一种对阿霉素耐药肿瘤细胞有活性的阿霉素甲氧基吗啉基衍生物）的体内抗肿瘤活性

In vivo anti-tumour activity of FCE 23762, a methoxymorpholinyl derivative of doxorubicin active on doxorubicin-resistant tumour cells.

作者信息

Ripamonti M, Pezzoni G, Pesenti E, Pastori A, Farao M, Bargiotti A, Suarato A, Spreafico F, Grandi M

机构信息

Research Center, Oncology Dept., Nerviano (MI), Italy.

出版信息

Br J Cancer. 1992 May;65(5):703-7. doi: 10.1038/bjc.1992.148.

DOI:10.1038/bjc.1992.148
PMID:1586598
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1977399/
Abstract

FCE 23762 is a new doxorubicin derivative obtained by appending a methoxymorpholinyl group at position 3' of the sugar moiety. The compound is greater than 80 times more potent than doxorubicin, it is highly lipophilic, and presents equivalent anti-tumour activity when administered by i.p., i.v. or oral route. The pattern of anti-tumour activity of FCE 23762 differs from that of doxorubicin in maintaining anti-tumour activity against two P388 murine leukaemia sublines resistant to doxorubicin and, although at borderline levels of efficacy, against LoVo human colon adenocarcinoma resistant to doxorubicin. FCE 23762 exhibits remarkable efficacy against MX-1 human mammary carcinoma, with most treated mice being cured both after i.v. and oral treatment. Anti-tumour activity was also observed against L1210 murine leukaemia and two sublines resistant to cis-platinum and melphalan, M5076 murine reticulosarcoma, MTV murine mammary carcinoma and N592 human small cell lung cancer.

摘要

FCE 23762是一种新的阿霉素衍生物，通过在糖部分的3'位连接一个甲氧基吗啉基而获得。该化合物的效力比阿霉素强80多倍，具有高度亲脂性，通过腹腔注射、静脉注射或口服途径给药时，具有同等的抗肿瘤活性。FCE 23762的抗肿瘤活性模式与阿霉素不同，它对两种对阿霉素耐药的P388小鼠白血病亚系保持抗肿瘤活性，并且尽管疗效处于临界水平，但对耐阿霉素的LoVo人结肠腺癌也有活性。FCE 23762对MX-1人乳腺癌显示出显著疗效，大多数接受治疗的小鼠在静脉注射和口服治疗后均被治愈。对L1210小鼠白血病以及对顺铂和马法兰耐药的两个亚系、M5076小鼠网状肉瘤、MTV小鼠乳腺癌和N592人小细胞肺癌也观察到了抗肿瘤活性。

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