129results about How to "Strong in vitro antitumor activity" patented technology

The invention discloses a 7-substituted-4-aryl coumarins compound, and a preparation method and an application thereof and belongs to the technical field of antitumor drugs. The 7-substituted-4-aryl coumarins compound is acquired in the manner of modifying and remolding 4 and 7 loci of the coumarins. The structural formula is shown in the specification. A pharmacological experiment proves that such a compound has an excellent antitumor activity, can be used for preparing the antitumor drugs, is capable of supplying a new selection for the development and application of the antitumor drugs and further can be applied to the design and optimization of the antitumor drugs. The preparation method of the compound has the advantages of easily acquired raw materials, mild reaction condition, easily realized synthesis method, simple reaction process and operation, low-cost reagents and higher yield.

The invention discloses a tripterine derivate and use thereof. The tripterine derivate has a structure as shown by a formula I. When R2 is H, R1 is alkyl, amine radical, alcohol, aryl, mixed aryl or heterocyclic radical connected with tripterine through ester bonds or amido bonds, and R2 is acyl or organic acid radical when R1 is OH. The tripterine derivate can be used for preparing anticancer medicine, anti-inflammatory medicine or medicine for treating central nervous system diseases. The medicine can be made into tablets, capsules, granules, fine grains, powder, pills, plaser, oral liquid or injections.

The invention relates to a class of diarylethene LSD1 / HDACs dual-target inhibitors containing a hydroxamic acid group, a preparation method and application thereof in the preparation of antitumor drugs, and belongs to the technical field of medicinal chemistry. Described compound has following general formula: wherein preferably 3-position or 4-position unit is substituted; R 2 OH, OCH are preferred 3 , F, H; R 3 Preferably H, CH 2 OH;R 4 Preferably H, CH 3 , F, OCH 3 ;R 5 H, OH, CH preferred 2 OH, CH 3 , F, OCH 3 ; X is N or CH; Y is N or CH. The compounds of the present invention have strong inhibitory activities on both LSD1 and HDAC1 / 6, and have good selectivity for LSD1, and a plurality of compounds have strong inhibitory effects on human colon cancer HCT-116 cell line and human gastric cancer MGC-803 cell line The in vitro antitumor activity is better than the marketed drug SAHA. It provides a basis for the research and development of LSD1 / HDACs dual-target inhibitor drugs, which can be used as candidates for further development or lead compounds for the development of anti-tumor therapeutic drugs.