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Anti-tumor activity of derivative of polyhalogenated isoquinoline imine

A technology of isoquinoline imines and derivatives, applied in the direction of antineoplastic drugs, organic active ingredients, drug combinations, etc., can solve the problems of high toxicity and side effects, poor selectivity, etc., and achieve a strong inhibitory effect

Inactive Publication Date: 2010-09-22
YUNNAN UNIV
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Problems solved by technology

However, the anti-tumor chemical drugs currently used in clinical practice generally have many problems such as poor selectivity, high toxicity and side effects, and easy drug resistance.

Method used

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  • Anti-tumor activity of derivative of polyhalogenated isoquinoline imine
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  • Anti-tumor activity of derivative of polyhalogenated isoquinoline imine

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Embodiment Construction

[0058] A total of 33 representative compounds of compounds I-A~I-G′ were used for pharmacological experiments. The tested human tumor cell line experiments: A431 (surface cancer), HL60 (leukemia), k562 (leukemia), HepG2 (liver cancer), Skov-3 (ovarian cancer). Cells were incubated with test compounds for 144 hours and cytotoxicity was measured using the MTT assay (Mosman, T. "A Rapid Colorimetric Test for Cell Growth and Survival: Applications to Proliferation and Cytotoxicity Assays"; J. Immunolog. Methods , 1983, 65, 66; Green, L.M., Rapid colorimetric assay for cell viability; application to quantification of cytotoxic and growth-inhibiting lymphokines, J.Immunolog.Methods, 1984, 70, 257-268.

[0059] The obtained data confirm that the compounds of the present invention have significant activity against epidermal cancer, leukemia, chronic myelogenous leukemia, liver cancer, ovarian cancer. The compound represented by the structure of formula (I) may be developed into a new...

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Abstract

The invention relates to a derivative of polyhalogenated isoquinoline imine with a structure shown in the formula (I) and cytotoxin activity of salt or solvate for medical purposes. The derivative of polyhalogenated isoquinoline imine with a structure shown in the formula (I) has stronger activity resisting against the growth of cells of epidermal carcinoma, leukemia, liver cancer, ovarian cancer, colon cancer and lung cancer tumors and can be used as an anti-tumor medicine in advance.

Description

technical field [0001] The invention relates to the fields of organic chemistry, medicinal chemistry and pharmacology, in particular, the invention relates to the cytotoxic activity of a class of polyhalogenated isoquinoline imine derivatives on tumor cells. Such compounds are found to have certain biological activity of inhibiting the growth of the tumor cells, and can be expected to be used as antitumor drugs. Background technique [0002] Tumors seriously threaten human life and health. Tumors are taking more and more ravages of human life. Therefore, the treatment and prevention of tumors has attracted widespread attention from the whole society. In the process of tumor treatment and prevention, chemotherapy, in which natural or synthetic compounds are used to block, reverse or prevent the occurrence of aggressive tumors, is the most widely used and effective clinical tumor treatment measure. However, the anti-tumor chemical drugs currently used in clinic generally ha...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4745A61K31/519A61P35/00A61P35/02
Inventor 严胜骄黄超林军曾祥慧
Owner YUNNAN UNIV
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