Use of compound in preparation of drugs for treatment and/or prevention of lung cancer, and composition of compound

A technology of compounds and compositions, applied in the fields of the use of compounds in the preparation of drugs for the treatment and/or prevention of lung cancer and their compositions, which can solve problems such as tumor recurrence and metastasis, and achieve excellent active effects

Active Publication Date: 2019-04-30
YUNNAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Many cancer patients have a remarkable curative effect in the initial stage of treatment, but with the prolongation of treatment time, cancer cells show strong drug resistance, and the tumor is prone to tumor recurrence and metastasis after drug resistance, so 80% to 90% of cancer patients Death is directly or indirectly attributable to tumor resistance to the drug

Method used

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  • Use of compound in preparation of drugs for treatment and/or prevention of lung cancer, and composition of compound
  • Use of compound in preparation of drugs for treatment and/or prevention of lung cancer, and composition of compound
  • Use of compound in preparation of drugs for treatment and/or prevention of lung cancer, and composition of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Activity analysis of compounds alone against paclitaxel-resistant lung adenocarcinoma cells

[0040] A549 / Taxol cells (5×10 3 / well) inoculated in 96-well cell culture plate, at 37°C in 5% CO 2 After culturing in a constant temperature incubator for 24h, then add the test samples of the concentrations shown in Table 1 to the cell culture in each well (dissolve paclitaxel, compound II, III and IV in 400 μl of DMSO respectively, and then configure The 0.1% DMSO solution of each compound to the required concentration was used as the test sample); the negative control was only adding DMSO to the cell culture to a volume concentration of 0.1%. Then place it in an incubator and incubate for 48h, add 20μl of MTS solution (purchased from Promega) and continue to incubate at 37°C for 1h, then measure the optical density (OD value) of each well at 490nm with a microplate reader to determine the living cells amount, and the inhibition rate was calculated. Calculation of IC usin...

Embodiment 2

[0046] Analysis of the activity of compounds combined with paclitaxel on paclitaxel-resistant lung adenocarcinoma cells

[0047] A549 / Taxol cells (5×10 3 / well) inoculated in 96-well cell culture plate, at 37°C in 5% CO 2 After cultivating in a constant temperature incubator for 24h, then add the test samples of the concentrations shown in Table 2 to the cell culture of each well (dissolve paclitaxel, compound II, III and IV in 400 μl of DMSO respectively, and then configure 0.1% DMSO solution of each compound mixture at the desired concentration was used as the test sample); the negative control was only adding DMSO to the cell culture to a volume concentration of 0.1%. Then place it in an incubator and incubate for 48h, add 20μl of MTS solution (purchased from Promega) and continue to incubate at 37°C for 1h, then measure the optical density (OD value) of each well at 490nm with a microplate reader to determine the living cells amount, and the inhibition rate was calculate...

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Abstract

The invention relates to a use of a compound in preparation of drugs for treatment and/or prevention of drug moderate lung cancer and/or drug-resistant lung cancer, and a composition of the compound,specifically, a use of the compound represented by a structural formula I and/or a pharmaceutically acceptable salt thereof in preparation of the drugs for treatment and/or prevention of lung cancer,wherein R1 and R6 are hydroxyl respectively, and R2, R3, R4 and R5 are selected independently from one of hydrogen, alkyl and hydroxyl; preferably, R2, R3, R4 and R5 are selected independently from hydrogen or alkyl; and more preferably, the alkyl is selected from one of methyl, ethyl and propyl.

Description

technical field [0001] The present invention relates to the use of the compound and / or its pharmaceutically acceptable salt in the preparation of drugs for the treatment and / or prevention of drug-resistant lung cancer, especially paclitaxel-resistant lung adenocarcinoma; the present invention also relates to the compound and paclitaxel pharmaceutical composition. Background technique [0002] Many cancer patients have a remarkable curative effect in the initial stage of treatment, but with the prolongation of treatment time, cancer cells show strong drug resistance, and the tumor is prone to tumor recurrence and metastasis after drug resistance, so 80% to 90% of cancer patients Death is directly or indirectly attributable to tumor resistance to the drug. The emergence of drug resistance is a complex process caused by multiple factors, including individual variation in patients and genetic differences in tumor cells. The mechanism of its generation includes, for example: 1)...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61K31/337A61P35/00
CPCA61K31/337A61K31/404A61P35/00A61K2300/00
Inventor 牛雪梅白雪黎胜红张克勤
Owner YUNNAN UNIV
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