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Quinone compounds and their uses for the treatment of cancer

A compound, cancer technology, applied in the field of 2,5-diaziridinylbenzoquinone compound, prodrug of cancer cells, cancer treatment, can solve problems such as poor solubility, hindering effective therapeutic preparations, increased cytotoxicity, etc.

Inactive Publication Date: 2015-04-29
ONCO NX
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although MeDZQ is bioreductively activated by DTD, it differs significantly from apaziquinone in that MeDZQ produces only a very slight increase in cytotoxicity under hypoxic conditions relative to aerobic conditions.
Furthermore, although a good correlation was shown between DTD activity and MeDZQ cytotoxicity in a series of human tumor cell lines, MeDZQ was hindered as an effective therapeutic agent due to its poor solubility.

Method used

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  • Quinone compounds and their uses for the treatment of cancer
  • Quinone compounds and their uses for the treatment of cancer
  • Quinone compounds and their uses for the treatment of cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0085] Materials and methods

[0086] Synthesis of Es5

[0087]

[0088] 1,4-Dimethoxy-2-methyl-benzene 2[1]

[0089]

[0090] Will be dissolved in diethyl ether (90cm 3 ) of 2,5-dimethoxytoluene 1 (9.0g, 59.21mmol) was dissolved in chloroform (30cm 3 ) in a stirred solution of iodine monochloride (10.17g, 62.65mmol). After adding 10% sodium thiosulfate (150cm 3 ), the mixture was stirred overnight. at 75cm 3 The organics were extracted twice with diethyl ether. Combine organics to saturate with NaHCO 3 Aqueous solution (150cm 3 ), salt water (100cm 3 ) washed, dried (MgSO 4 ) and dried under reduced pressure. The final solid was recrystallized from methanol to give the title compound 2 as a red solid (11.3 g, 69%).

[0091] R f 0.52 (SiO 2 , Hex 3:1 EtOAc).

[0092] Mp 80-82°C (literature 81-82°C (Reed et al., JACS, 120(38):9729-9734, 1998).

[0093] 1 H NMR (400MHz, CDCl 3 )2.12 (3H,s,CH 3 ),3.72(3H,s,OCH 3 ),3.75(3H,s,OCH 3 ), 6.60 (1H, s, ArH)...

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Abstract

Quinone Compounds and Their Uses for the Treatment of Cancer Quinone compounds having useful therapeutic activity such as anticancer activity, and compositions comprising such compounds, are described. The use of such compounds and compositions in the treatment of cancer is also described.

Description

[0001] This application is related to British patent application GB 1213486.2 filed on July 30, 2012, the entire contents of which are incorporated herein by reference. technical field [0002] The invention relates to a quinone compound and its medicinal use, especially for cancer treatment. More particularly, the present invention relates to 2,5-diaziridinylbenzoquinone compounds, which are prodrugs that can activate cancer cells expressing DT-diaphorase. Background technique [0003] DT-diaphorase (DTD) is an enzyme that is overexpressed in various types of cancer tissues, including breast tumors, colon tumors, liver tumors, bladder tumors, gastric tumors, central nervous system (CNS ) tumors and lung tumors, and melanoma. Various quinone-based prodrugs have been studied to determine their effects on DTD-expressing cancer cells. For example, the expression of DTD was increased 80-fold in primary non-small cell lung cancer (NSCLC) relative to normal lung tissue, and 400-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/10A61K31/495A61P35/00A61K33/243
CPCC07D203/14A61K33/243C07D403/10A61K31/337A61K31/396A61K31/407A61P35/00A61P35/02A61P43/00A61K31/495A61K31/122
Inventor 阿兰·麦戈恩约翰·哈德菲尔德约翰·巴特勒
Owner ONCO NX
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