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多卡霉素SA及其衍生物的研究。

Studies on duocarmycin SA and its derivatives.

作者信息

Nagamura S, Asai A, Kobayashi E, Gomi K, Saito H

机构信息

Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.

出版信息

Bioorg Med Chem. 1997 Mar;5(3):623-30. doi: 10.1016/s0968-0896(96)00276-3.

DOI:10.1016/s0968-0896(96)00276-3
PMID:9113339
Abstract

New duocarmycin SA derivatives have been synthesized and evaluated for in vitro anticellular activity against HeLa S3 cells, and in vivo antitumor activity against murine sarcoma 180 in mice. The results suggested that the N,N-dialkylcarbamoyl derivatives bearing the p-methoxy cinnamoyl group, which was prepared from duocarmycin SA, showed good in vivo antitumor activities superior to native duocarmycin SA.

摘要

已经合成了新型的多卡霉素SA衍生物,并对其针对HeLa S3细胞的体外抗细胞活性以及针对小鼠肉瘤180的体内抗肿瘤活性进行了评估。结果表明,由多卡霉素SA制备的带有对甲氧基肉桂酰基的N,N-二烷基氨基甲酰基衍生物显示出优于天然多卡霉素SA的良好体内抗肿瘤活性。

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1
Studies on duocarmycin SA and its derivatives.多卡霉素SA及其衍生物的研究。
Bioorg Med Chem. 1997 Mar;5(3):623-30. doi: 10.1016/s0968-0896(96)00276-3.
2
Synthesis and antitumor activity of duocarmycin derivatives: A-ring pyrrole compounds bearing cinnamoyl groups.柔红霉素衍生物的合成及其抗肿瘤活性:带有肉桂酰基的A环吡咯化合物。
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Synthesis and antitumor activity of duocarmycin derivatives.多卡霉素衍生物的合成与抗肿瘤活性
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Synthesis and antitumor activity of duocarmycin derivatives: modification of segment A of duocarmycin B2.
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Synthesis and antitumor activity of duocarmycin derivatives: A-ring pyrrole compounds bearing beta-(5',6',7'-trimethoxy-2'-indolyl)acryloyl group.
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Bifunctional alkylating agents derived from duocarmycin SA: potent antitumor activity with altered sequence selectivity.源自多卡霉素SA的双功能烷基化剂:具有改变的序列选择性的强效抗肿瘤活性。
Bioorg Med Chem Lett. 2000 Mar 6;10(5):495-8. doi: 10.1016/s0960-894x(00)00042-1.
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New water-soluble duocarmycin derivatives: synthesis and antitumor activity of A-ring pyrrole compounds bearing beta-heteroarylacryloyl groups.新型水溶性多卡霉素衍生物:含β-杂芳基丙烯酰基的A环吡咯化合物的合成与抗肿瘤活性
J Med Chem. 1999 Feb 25;42(4):669-76. doi: 10.1021/jm980559y.

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