Application of N-heteroaryl phenylamine compounds for preparation of antitumor drugs
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A technology of heteroarylaniline and antitumor drug, which is applied in the application field of N-heteroarylaniline compound as antitumor drug, and can solve the problems such as the report that the compound has no antitumor drug application.
Active Publication Date: 2016-01-27
SHENYANG RES INST OF CHEM IND
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[0005] In the prior art, there is no report on the application of the compound as shown in the general formula I of the present invention as an antitumor drug
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Embodiment 1
[0108] Example 1: The growth inhibition rate of human bladder cancer cells J82, T24, prostate cancer cells LNCap, PC-3, lung cancer cells A549, H460, using in vitro cell culture technology, about 1,000 to 3,000 of the above different cancer cells were implanted In a 24-well plate, then add 1 ml of cell culture medium well known to those skilled in the art to be able to cultivate test tumor cell lines into each well, and place it in a cell incubator (CO 2 5%, 370°C) after 24 hours of incubation, then add the appropriate concentration of the control drug and the prepared substance to be tested into the well. Note that the volume of the added solution does not exceed 0.5% of the total volume. Let the cells continue to grow in the cell incubator. After a week, aspirate the cell culture solution and wash once with cold 1 ml PBS. Then, fix with 1% formalin for 10 minutes at room temperature, and then wash once with cold 1 ml PBS. Add 0.1% crystal violet for 30 minutes. Crystal viole...
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Abstract
The invention discloses an application of N-heteroaryl phenylamine compounds for preparation of antitumor drugs; the N-heteroaryl phenylamine compounds are represented by the general formula I, wherein in the formula, definitions of all substituents are shown in the description. The compounds represented by the general formula (I) have good antitumor activity, and especially have excellent activity on lung cancer A549 and H460, bladder cancer T24 and J82, prostatic cancer LNCap and PC-3 and the like.
Description
Technical field [0001] The invention belongs to the field of medicine and relates to the field of anti-tumor drugs. Specifically, it relates to the application of an N-heteroarylaniline compound as an antitumor drug. Background technique [0002] Patent CN102827072, DE3905238, DE3716512, DE3618353, EP31257, EP476607, EP139613, GB2137991, JP11209205, JP61189204, JP61072755, JP60064963, JP57058667, JP56030963, JP56065804, US4694009, US4659363, US4840662 and journals NipponNoyaku 90 and ACSSymposium Series (1995), 584 (Synthesis and Chemistry of Agrochemicals IV), 443-8, etc. reported that N-heteroaryl anilines have agricultural bactericidal, acaricidal or insecticidal activities. [0003] Patent WO2012146933 reports that the agricultural fungicide fluazinam has anticancer activity. [0004] [0005] In the prior art, there is no report of the compound whose structure is represented by the general formula I of the present invention as an antitumor drug. Summary of the invention [000...
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