New use of pyrrolopyridine derivative compounds for prevention and/or treatment of cancer
A compound and cancer technology, applied in the direction of drug combinations, antibody medical ingredients, medical preparations containing active ingredients, etc., can solve problems such as cytotoxicity, achieve the effects of treating or preventing cancer, excellent in vivo stability, and reducing resistance
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experiment example 1
[0082] Evaluation of Inhibitory Activities of Compounds According to the Present Invention to Various Kinases
[0083] The measurement of the enzyme (kinase) selectivity and inhibitory activity of compound 1 selected from the exemplary compounds of the present invention was entrusted to DiscoverX, and the experiment was performed using the scanMAXTM kinase analysis panel. Here, the concentration of the drug used to treat the enzyme was 1 μM in DMSO. The control percentage (control %) was determined using the following method, and the results are shown in Table 2.
[0084] [(Example Compound – Positive Control) / (Negative Control – Positive Control)×100]
[0085] Here, a positive control refers to a compound exhibiting a control percentage of 0%, while a negative control represents a control percentage of 100% in the case of DMSO. Further, for the enzyme selectivities of the present invention, [compound] is judged to be active against that enzyme if the percentage of control ...
experiment example 3
[0095] Comparison of protein kinase expression in non-small cell lung cancer cell lines and non-small cell lung cancer cell lines resistant to EGFR-targeted drugs
[0096] To compare the expression of DYRK1A in non-small cell lung cancer cell lines and non-small cell lung cancer cell lines with gefitinib resistance, a western blot test was performed. Cells were treated with 1X RIPA buffer supplemented with protease inhibitors and phosphatase inhibitors, then recovered and subsequently lysed on ice for 30 minutes and centrifuged at 14000 rpm and 4°C for 15 minutes. The supernatant was separated and the protein was quantified using the Bradford assay. Western blot tests were performed using the same amount of protein. React with the corresponding primary antibody at 4°C for 16 hours, and then react with the secondary antibody. Use LAS500 to detect the results.
[0097] It was found that, compared with the PC9 human non-small cell lung cancer cell line ( figure 2 ) compared...
experiment example 5
[0104] It was found that, if image 3 and Figure 4 showed that concomitant use of [these compounds] with Compound 1 of the present invention significantly reduced lung cancer (PC-9) cells compared to single administration of EGFR-targeted drugs (gefitinib or osimertinib), and The rate of cancer cell regrowth was demonstrated to be reduced, allowing for continuation of treatment. That is, while in the case of single treatment with an EGFR-targeting drug, early regeneration of cancer cells was observed during the treatment period, in the case of treatment with the compounds of the present invention, an increase in cancer cells was found in a concentration-dependent manner. continues to be suppressed. This suggests that concomitant administration of the compounds of the present invention also has an effect on the resistance (tolerance) of cancer cells to EGFR-targeting drugs. Further, although no anticancer effect on lung cancer cells was observed for single treatment with Co...
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