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A new series of ellipticine derivatives (1-(alkylamino)-9-methoxyellipticine). Synthesis, DNA binding, and biological properties.

作者信息

Larue L, Rivalle C, Muzard G, Paoletti C, Bisagni E, Paoletti J

机构信息

CNRS (LA 147), Institut Gustave Roussy, Villejuif, France.

出版信息

J Med Chem. 1988 Oct;31(10):1951-6. doi: 10.1021/jm00118a014.

DOI:10.1021/jm00118a014
PMID:3172128
Abstract

A new series of ellipticine derivatives, 1-(alkylamino)-5,11-dimethyl-9-methoxy-6H-pyrido[4,3-b]carbazoles, were synthesized as potential DNA intercalating antitumor drugs. The structure of these compounds were confirmed by 1H NMR spectroscopy and mass spectrometry. These compounds are able to bind to DNA with an affinity of about 10(6) M-1, and their intercalating characteristics (lengthening and unwinding of DNA) depend upon the length of the chain in position 1. The cytotoxicities of these compounds on L1210 and NIH-3T3 cells are quite similar, and fluorescence techniques showed that the compounds are localized mainly in the cytoplasmic granules of the cells. One of these compounds appears to show a very high antitumor activity (equivalent to the more active known ellipticine analogues: 10-[[gamma-(diethylamino)propyl]amino]-6-methyl-5H- pyrido[3',4':4,5]pyrollo[2,3-g]isoquinoleine (BD40), 1-[[gamma-(diethylamino)propyl]amino]-9-methoxyellipticine (BD84) and 2-[beta-(diethylamino)ethyl]-9-hydroxyellipticinium chloride (DEAE).

摘要

相似文献

1
A new series of ellipticine derivatives (1-(alkylamino)-9-methoxyellipticine). Synthesis, DNA binding, and biological properties.
J Med Chem. 1988 Oct;31(10):1951-6. doi: 10.1021/jm00118a014.
2
Interrelationship between affinity for DNA, cytotoxicity and induction of DNA-breaks in cultured L1210 cells for two series of tricyclic intercalators. Simplified analogues of ellipticine derivatives.
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Synthesis of 11H-pyridocarbazoles and derivatives. Comparison of their DNA binding and antitumor activity with those of 6H- and 7H-pyridocarbazoles.
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Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.一系列新合成的1-氨基取代椭圆玫瑰树碱衍生物的构效关系
J Med Chem. 1980 Nov;23(11):1212-6. doi: 10.1021/jm00185a012.
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Physicochemical and pharmacological properties of the antitumor ellipticine derivative 2-(diethylamino-2-ethyl)9-hydroxy ellipticinium-chloride, HCl.抗肿瘤椭圆玫瑰树碱衍生物2-（二乙氨基-2-乙基）-9-羟基氯化玫瑰树碱（HCl）的物理化学和药理学性质
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Antitumor amino-substituted pyrido[3',4':4,5]pyrrolo[2,3-g]isoquinolines and pyrido[4,3-b]carbazole derivatives: synthesis and evaluation of compounds resulting from new side chain and heterocycle modifications.抗肿瘤氨基取代的吡啶并[3',4':4,5]吡咯并[2,3-g]异喹啉和吡啶并[4,3-b]咔唑衍生物：新侧链和杂环修饰所得化合物的合成与评价
J Med Chem. 1983 Feb;26(2):181-5. doi: 10.1021/jm00356a012.
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Ellipticine derivatives with an affinity to the estrogen receptor, an approach to develop intercalating drugs with a specific effect on the hormone-dependent breast cancer.具有雌激素受体亲和力的椭圆玫瑰树碱衍生物，一种开发对激素依赖性乳腺癌有特定作用的嵌入药物的方法。
J Med Chem. 1985 Jun;28(6):752-61. doi: 10.1021/jm00383a011.
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Synthesis and evaluation of 4-amino-substituted 7-methoxy (and 7-hydroxy)- 11-methyl (and 5,11-dimethyl)-10H-pyrido [2,3-b] carbazoles and 4-amino- substituted 11-methyl (and 5,11-dimethyl)-10H-pyrido[3',4':4,5] pyrrolo [3,2-g] quinolines, two new series related to antitumor ellipticine derivatives.4-氨基取代的7-甲氧基（及7-羟基）-11-甲基（及5,11-二甲基）-10H-吡啶并[2,3-b]咔唑和4-氨基取代的11-甲基（及5,11-二甲基）-10H-吡啶并[3',4':4,5]吡咯并[3,2-g]喹啉的合成与评价，这是两个与抗肿瘤椭圆玫瑰树碱衍生物相关的新系列。
Anticancer Drug Des. 1993 Dec;8(6):399-416.
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Synthesis and evaluation of 9-hydroxy-5-methyl-(and 5,6-dimethyl)-6H-pyrido[4,3-b]carbazole-1-N- [(dialkylamino)alkyl]carboxamides, a new promising series of antitumor olivacine derivatives.新型有前景的抗肿瘤橄榄喜树碱衍生物系列9-羟基-5-甲基-（及5,6-二甲基）-6H-吡啶并[4,3-b]咔唑-1-N-[(二烷基氨基)烷基]羧酰胺的合成与评价
J Med Chem. 1994 Jul 22;37(15):2445-52. doi: 10.1021/jm00041a024.

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