Camptothecin derivatives and their application in the preparation of antitumor drugs

A technology of tumor drugs and derivatives, applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of difficult to formulate drugs, biological toxicity, and difficult to predict biological properties, and achieve good efficacy, low toxicity, and excellent in vitro biological properties. active effect

Inactive Publication Date: 2020-01-07
深圳瀜新生物科技有限公司
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Problems solved by technology

Although a large number of literatures have reported a variety of modification strategies for camptothecin and achieved certain results, its specific structure-activity relationship is still unclear, and it is difficult for people to predict its biological properties based on the structure of the derivative, especially is its biological toxicity
[0008] In addition, the existing camptothecin derivatives have poor water solubility and stability, making it difficult to make medicines, which limits their application

Method used

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  • Camptothecin derivatives and their application in the preparation of antitumor drugs
  • Camptothecin derivatives and their application in the preparation of antitumor drugs
  • Camptothecin derivatives and their application in the preparation of antitumor drugs

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Embodiment Construction

[0029] Related definitions:

[0030] 1. Pharmaceutically acceptable salts

[0031] "Pharmaceutically acceptable" as used herein means lack of unacceptable toxicity in a compound such as a salt or an excipient. Basic compounds are capable of forming different forms of salts with various acids that are used to prepare pharmaceutically acceptable salts. The inorganic anions of these salts include, but are not limited to, sulfate, bisulfate, sulfite, Nitrate, nitrite, chloride, bromide, iodide, phosphate, (one, two) hydrogen phosphate, isonicotinic acid, etc.; organic anions include acetate, lactate, oxalate, maleate, citrate Citrate, Salicylate, Cinnamate, Oleate, Fumarate, Tartrate, Pyruvate, Tanninate, Trifluoroacetate, Propionate, Citrate, Pantothenate, Ascorbate, Succinate salt, fumarate, gluconate, glucuronate, sucrose salt, formate, benzoate, glutamate, methanesulfonate, ethanesulfonate, benzenesulfonate, toluenesulfonate , Pamoate, etc.

[0032] The inventive acidic co...

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Abstract

The invention discloses a class of novel camptothecin derivatives and applications in preparation of antitumor drugs. According to the present invention, the camptothecin derivative exhibits excellentin vitro biological activity in the inhibition of gastric cancer, liver cancer, breast cancer and neuroblastoma, and the mouse in vivo liver cancer bioactivity test results show that the camptothecinderivative provides good treatment effect, low toxicity and good water solubility compared to the commercial drug topotecan; and the data and analysis results prove that the prepared novel camptothecin / topotecan derivative has advantages of toxicity reducing and bioactivity improving compared to the commercial drug topotecan, such that the camptothecin derivatives as a class of the new low-toxicity and high-efficiency candidate drugs have wide application prospect.

Description

technical field [0001] The invention relates to a novel camptothecin derivative and its application in the preparation of antitumor drugs. Background technique [0002] Cancer is currently the number one killer of human health. According to statistics released by the Ministry of Health in 2010, malignant tumors have become the leading cause of death in China, and more than 1 million patients die of tumors every year. According to the statistics of the World Health Organization (WHO), nearly 700,000 people die of malignant tumors in the world every year on average, and about 8.7 million new cases are reported, and they are still increasing every year. Cerebrovascular disease. Therefore, the treatment of cancer is urgent. [0003] Camptothecin (CPT) is a cytotoxic alkaloid extracted from Camptotheca involucrata in 1966, and its structural formula is as follows: [0004] [0005] Camptothecin belongs to tryptophan-terpene alkaloids. Tumor experiments have proved that thi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D498/22A61K31/4375A61K31/444A61P35/00
CPCC07D498/22
Inventor 余慧东黄湧李希建侯廷军潘培辰岑国亮
Owner 深圳瀜新生物科技有限公司
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