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Preparation method and application of benzo[c] carbazole amide compound

A carboxamide compound and compound technology, which are applied in the field of benzo[c]carbazole-5-carboxamide compounds, can solve problems such as hypotension and hypersensitivity, and achieve the effects of low toxicity, high activity and good solubility

Inactive Publication Date: 2014-10-15
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Some common toxicities of etoposide include bone marrow suppression, nausea, vomiting, hair loss, and the most serious side effect is the occurrence of acute myeloid leukemia, and in the use of etoposide (or teniposide) injection, often Can cause hypotension and hypersensitivity

Method used

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  • Preparation method and application of benzo[c] carbazole amide compound
  • Preparation method and application of benzo[c] carbazole amide compound
  • Preparation method and application of benzo[c] carbazole amide compound

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Embodiment Construction

[0028] The present invention will be further explained below in conjunction with examples, but these examples are by no means any limitation to the present invention. In all embodiments, the melting point is measured with a WRS-1B digital melting point apparatus, and the thermometer is uncorrected; 1 H NMR was recorded by a Brucher AM-400 nuclear magnetic resonance instrument, and the chemical shift was expressed in δ (ppm); the silica gel used for separation was 400 mesh.

[0029] Preparation Example

[0030] Preparation of Compound 2:

[0031]

[0032] Add LiAlH to a 100mL two-necked bottle under nitrogen protection 4 (2.6g, 66mmol) and 30mL tetrahydrofuran solution, and placed in an ice bath, compound 1 (5.0g, 26mmol) was dissolved in 20mL tetrahydrofuran, and slowly added dropwise to the reaction flask under nitrogen protection. After the dropwise addition, the ice bath was removed, and the mixture was stirred overnight at room temperature. After the reaction, the r...

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Abstract

A benzo[c] carbazole amide compound is a potential novel antitumor drug, and a like structure is proved to have better inhibiting effect on certain tumors. However, reported methods for synthesizing like compounds have the defects of long reaction route, low total yield and the like. A preparation method provided by the invention adopts benzyne as a synthetic building block, a benzo[c] carbazole maternal nuclear is synthesized successfully and efficiently in a few steps, and possibilities are provided for efficient screening of the kind of drugs. The invention further provides a synthesized benzo[c] carbazole-5-formamide compound represented in the general formula (I) and the activity and an application of the compound as an antitumor drug.

Description

technical field [0001] The invention relates to a class of benzo[c]carbazole-5-carboxamide compounds, a preparation method thereof and an application as an antitumor drug. Background technique [0002] In today's society, cancer occurs frequently, and malignant tumors have seriously affected human health and threatened human life. DNA topoisomerase is an important ribozyme in cells, which mainly changes the topological structure of DNA through catalytic action. Topoisomerases in eukaryotic cells are mainly divided into topoisomerase I and topoisomerase II. Topoisomerase II plays an important role in important life processes such as cell DNA replication, transcription and mitosis. Based on the understanding of the key role of topoisomerase II in cells, research on this type of compound has always been one of the hot spots in the development of anti-tumor drugs. Currently listed topoisomerase II inhibitors include etoposide, teniposide, doxorubicin, idarubicin, epirubicin an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/80A61K31/5377A61K31/454A61K31/403A61P35/00A61P1/00A61P11/00
CPCC07D209/80
Inventor 沙风伍新燕陶源张飞汤晨宇袁晶周晨张南
Owner EAST CHINA UNIV OF SCI & TECH