208167-83-3Relevant academic research and scientific papers
Natural product-based design, synthesis and biological evaluation of anthra[2,1-d]thiazole-6,11-dione derivatives from rhein as novel antitumour agents
Liang, Yu-Kun,Yue, Zhi-Zhou,Li, Jia-Xin,Tan, Cun,Miao, Ze-Hong,Tan, Wen-Fu,Yang, Chun-Hao
, p. 505 - 515 (2014)
Two series of novel 2-substituted 5,7-dihydroxyanthra[2,1-d]thiazole-6,11- dione derivatives from natural rhein were designed, synthesized and evaluated for their antitumour activities against human cancer cell lines A549 and HeLa in vitro.
Preparation method of 4-morpholinyl-2-ethylpiperazine
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Paragraph 0052; 0054; 0057; 0059; 0062; 0064, (2020/03/25)
The invention discloses a preparation method of 4-morpholinyl-2-ethylpiperazine. The method comprises the following steps: (1) putting 2-hydroxyethylpiperazine and thionyl chloride into a first solvent, and performing a reaction to convert hydroxyl groups into chlorine to obtain a first reaction product; (2) putting the first reaction product obtained in step (1) and boc anhydride into a second solvent, and performing a reaction to obtain an N-boc protected second reaction product; (3) putting the second reaction product obtained in step (2), morpholine and an acid-binding agent into a third solvent at 20-50 DEG C, and performing a reaction to obtain a third reaction product; and (4) dissolving the third reaction product obtained in step (3) and an alkali in a fourth solvent, heating the obtained solution to 40-80 DEG C, performing a reaction for about 10-20 h, concentrating the obtained reaction solution, and extracting and concentrating the obtained concentrate to obtain the 4-morpholinyl-2-ethylpiperazine. Raw materials used in the method are cheap and are easy to obtain, the operation process is simple, and the purity of the obtained product is high and exceeds 99%.
N-(3-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PHENYL)BENZAMIDE DERIVATIVES
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Page/Page column 126; 127, (2019/10/23)
The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
A anthraquinone and thiazole compounds, its preparation method and use thereof
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, (2017/08/10)
The invention relates to a compound which takes 5,7-dihydroxyanthraquinone [2,1-d]thiazole as a mother nucleus, which has a following general formula, and relates to a preparation method and an application of the compound in an antitumor drug. The compound takes a traditional natural product rheinic acid as an initial raw material, and a series of compound with high antineoplastic activity is synthesized through mild reaction condition. The antitumor activity in vitro of the preferable compound is stronger by more than 30 times by comparing with rheinic acid.
Compound and application of compound to treating colon cancer
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, (2017/11/04)
The invention discloses a compound and application of the compound to treating the colon cancer. The structural formula of the compound is shown in the formula I, wherein R1, R2, R3 and R4 in the formula I are respectively independently chosen from alkyl groups and alkoxy groups, the number of hydrogen atoms, halogen, nitro and carbon atoms in the alkyl group is 1-6, the number of carbon atoms in the alkoxy group is 1-6, R5 is chosen from nitro and -NR6R7, wherein R6 and R7 are respectively independently the hydrogen atom or CH2Ar, the Ar represents a phenyl group or an aryl group, the para-position of the aryl group is substituted by R8, the aryl group is a phenyl group, the R8 is an alkoxy group or the following shown groups, and the number of halogen, hydroxyl and carbon atoms in the R8 is 1-6. The compound also has an obvious effect on inhibiting a tumor sphere from a cancer patient with the colon cancer. In addition, the compound also has an obvious effect on inhibiting the migration and the moving ability of a colon cancer cell line. A novel medicine for treating the colon cancer is expected to be developed on the basis of the compound.
Compounds and methods for inhibiting phosphate transport
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Page/Page column 163; 237, (2016/05/02)
Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Design, synthesis and biological evaluation of novel podophyllotoxin derivatives bearing 4β-disulfide/trisulfide bond as cytotoxic agents
Zhu, Shi-Jun,Ying, Hua-Zhou,Wu, Yan,Qiu, Ni,Liu, Tao,Yang, Bo,Dong, Xiao-Wu,Hu, Yong-Zhou
, p. 103172 - 103183 (2015/12/23)
A novel series of C-4β-disulfide/trisulfide-containing podophyllotoxin derivatives were designed, synthesized, and biologically evaluated for their cytotoxic activities against human cancer cell lines, including KB (Mouth Epidermal Carcinoma Cells) and KB/VCR (Vincristine-resistant Mouth Epidermal Carcinoma Cells). Most of these compounds exhibited promising moderate to good cytotoxic activities. In particular, some of them displayed even superior activities to that of etoposide, especially for KB/VCR cell lines, indicating that introduction of the disulfide/trisulfide moiety would be beneficial for overcoming the multi-drug resistant limitation of etoposide. Moreover, the metabolic evaluation of the most promising compound was further performed to reveal that disulfide bond can be stable in human plasma over 8 hours, indicating good potential of these compounds for in vivo anti-cancer activities.
NOVEL CYCLOSPORIN DERIVATIVES AND USES THEREOF
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, (2014/09/29)
The present invention relates to a compound of the Formula (I)): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, and hair loss.
BICYCLIC PYRIMIDINONES AND USES THEREOF
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Page/Page column 89, (2008/12/06)
The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compoundof Formula I is also provided.
SUBSTITUTED BENZYLIMIDAZOLES USEFUL FOR THE TREATMENT OF INFLAMMATORY DISEASES
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, (2008/06/13)
The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory conditions.
