Furazan derivative of coumarin parent nucleus and antineoplastic activity

A technology of coumarin and derivatives, which is applied in the direction of antineoplastic drugs, organic active ingredients, drug combinations, etc., can solve the problems of drug resistance, reduced selectivity, and severe toxic and side effects, and achieve the activity inhibition of tumor cells, The effect of novel structure
CN105153142AActive Publication Date: 2015-12-16FUDAN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
FUDAN UNIV
Publication Date
2015-12-16

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Abstract

The invention belongs to the field of pharmaceutical chemistry, and relates to a furazan derivative which is prepared by combining a coumarin parent nucleus and an isomer of the coumarin parent nucleus with a furazan oxide through linking of groups with different lengths and structures. It is proved by the experiments that the furazan derivative has excellent effects on inhibiting sensitive human tumour cells and drug-resistant tumor strains, and on inhibiting activity of normal growth of HUVEC for measuring an inhibiting action of neovascularization, and on inhibiting activity of cell proliferation of cis-platinum-resistant A2780 cell strains and gemcitabine-resistant HM231 cell strains. It is shown by an initial pharmacological mechanism that by releasing nitric oxide with the high concentration, the furazan derivative can induce apoptosis of cancer cells, inhibits MEK activity, and obviously inhibits phosphorylation of MEK in an MAPK/ERK channel, thereby generating a significant effect on inhibiting growth of a tumor. According to the composition in the invention, excellent basis for obtaining candidate medicines having inhibition activity of sensitive and drug-resistant tumors and for illustrating the pharmacological action is provided.
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Claims

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