Application of a compound in the preparation of mTOR inhibitors

A technology of compounds and inhibitors, applied in the field of mTOR inhibitors, compounds as mTOR inhibitors, can solve the problems of large toxic side effects, instability, high toxicity, etc., and achieve the effect of controlling proliferation

Active Publication Date: 2017-10-27
绍兴康岳生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although some compounds have been reported in the prior art that can inhibit mTOR signal transduction, there are many toxic side effects and poor pharmacological parameters (such as high toxicity to normal cells and instability in aqueous phase), thus limiting their application

Method used

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  • Application of a compound in the preparation of mTOR inhibitors
  • Application of a compound in the preparation of mTOR inhibitors
  • Application of a compound in the preparation of mTOR inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 SC06 inhibits the proliferation of myeloma and leukemia cell lines and lymphoma cell lines

[0032] Different multiple myeloma cell lines (RPMI-8226, JJN3, KMS11, LP1, OCI-My5, OPM2, U266), leukemia cell lines (AML2, K562, NB4, THP1) and lymphoma cell lines (Jurkat) were tested by SC06 (20 μM, the drug was prepared with 100% DMSO and diluted in 0.5% DMSO solution) after 72 hours of treatment, add thiazolium blue (MTT) for 2 to 4 hours, add MTTbuffer, read the plate after overnight incubation to calculate the cell survival rate (per group of cells in triplicate wells). attached figure 1 This is the cell survival curve (MTT) graph of different myeloma and leukemia cell lines treated with SC06. It can be seen that SC06 can effectively inhibit the proliferation of multiple myeloma cells and leukemia cells and induce tumor cell apoptosis.

Embodiment 2

[0033] Example 2 SC06 inhibits the growth of solid tumor cell lines

[0034] Different solid tumor cell lines (lung cancer (A549, H460), cervical cancer (HeLa), prostate cancer (PC3), ovarian cancer (SKOV3), breast cancer (T47D) were treated with SC06 (20 μM, the drug was prepared with 100% DMSO Diluted in 0.5% DMSO solution) after treatment for 72 hours, photographed with an inverted fluorescence microscope. Attached figure 2 Microscopic images of different solid tumor cell lines treated with SC06. It can be seen that SC06 can effectively inhibit the proliferation of various tumor cells and induce tumor cell apoptosis.

Embodiment 3

[0035] Example 3 SC06 inhibits the phosphorylation of mTOR

[0036] Different multiple myeloma cell lines (LP1, OPM2, JJN3 and RPMI-8226) were treated with SC06 (20 μM, the drug was prepared in 100% DMSO and diluted in 0.5% DMSO solution) for 24 hours, the cells were collected, and the total protein, the expression of phosphorylated mTOR (p-mTOR) and total mTOR was detected by Western blot; attached image 3 It is the western blot (Western Blot) figure after different tumor cells are treated, SC06 can significantly inhibit the phosphorylation level of mTOR, showing a significant inhibitory effect on it.

[0037] Different tumor cells were cultured overnight in low serum (0.5%), treated with SC06, S14161 and rapamycin (Rapamycin) (10 nM) for 2 hours, then treated with insulin-like growth factor (IGF-1) for 15 minutes, and the cells were collected. The total protein was extracted, and the expression of phosphorylated mTOR (p-mTOR) was detected by Western blot. GAPDH was used as...

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Abstract

The invention discloses an application of a compound in the preparation of an mTOR inhibitor, which belongs to the field of medicine, and specifically relates to the application of the compound SC06 in the preparation of an mTOR inhibitor; the compound has the ability to inhibit the mTOR signaling pathway to induce tumor apoptosis, inhibit function of tumor growth. The compound SC06 of the present invention can not only inhibit the proliferation and growth of tumor cells, but also more effectively induce the apoptosis of tumor cells, thereby exhibiting a therapeutic effect on tumors.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to an mTOR inhibitor, in particular to the application of a compound as an mTOR inhibitor. Background technique [0002] At present, tumors are increasingly threatening human life and health. In 2012, my country released the annual report on tumor incidence registration for the first time. The annual report shows that there are about 3.12 million new cancer cases in my country every year, among which, the national average is 8550 people every day, and 6 people are diagnosed with tumors every minute. At the same time, the national cancer mortality rate is 1.8054 / 100,000, with 2.7 million cases of cancer death every year. Among them, the probability of death due to tumors among Chinese residents is 13%, that is, 1 out of every 7 to 8 people dies due to tumors. In addition to the morbidity, the reason for the high mortality rate of tumors is the lack of effective anti-tumor drugs. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4439A61P35/00A61P35/02C07D401/12
Inventor 毛新良韩昆昆
Owner 绍兴康岳生物科技有限公司
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