39053-41-3Relevant articles and documents
Preparation method and application of tetrahydrobenzothiophene compound and pharmaceutical composition
-
Paragraph 0169; 0172-0173; 0241; 0244-0245, (2021/10/16)
The invention belongs to the field of medicines, and particularly relates to a tetrahydrobenzothiophene compound as well as a pharmaceutical composition and a preparation method and application thereof. The tetrahydrobenzothiophene compound is a compound I as shown I. In-flight R1 And R2 The C1 -4 is a saturated/unsaturated hydrocarbon group. - OCH3 , OCH2 CH3 Phenyl, substituted phenyl, NO2 One - COR of - OH - F, Cl - Br. I - H R1 AND R2 Or different. R3 It is-F. - Cl, Br, I, OH, Amino, C1 -4 saturated/unsaturated hydrocarbon group, OCH3 , OCH2 CH3 , H, Wherein one of them is, n ≥ 5, n Being an integer. The compound effectively inhibits salmonella by inhibiting the synthesis of ATP-dependent transporter in the lipopolysaccharide synthesis pathway. Aeruginosa, escherichia coli and staphylococcus aureus.
Synthesis and Antiproliferative Activities of Novel Substituted 5-Anilino-α-Glucofuranose Derivatives
Hou, Qiaoli,Li, Baolin,Li, Xiabing,Sun, Baoli,Wang, Lili,Wang, Wei,Zhang, Yaling
, (2020/05/05)
In order to find novel antitumor candidate agents with high efficiency and low toxicity, 14 novel substituted 5-anilino-α-glucofuranose derivatives have been designed, synthesized and evaluated for antiproliferative activities in vitro. Their structures were characterized by NMR (1H and 13C) and HR-MS, and configuration (R/S) at C(5) was identified by two-dimensional 1H,1H-NOESY-NMR spectrum. Their antiproliferative activities against human tumor cells were investigated by MTT assay. The results demonstrated that most of the synthesized compounds had antiproliferative effects comparable to the reference drugs gefitinib and lapatinib. In particular, (5R)-5-O-(3-chloro-4-{[5-(4-fluorophenyl)thiophen-2-yl]methyl}anilino)-5-deoxy-1,2-O-(1-methylethylidene)-α-glucofuranose (9da) showed the most potent antiproliferative effects against SW480, A431 and A549 cells, with IC50 values of 8.57, 5.15 and 15.24 μm, respectively. This work suggested 5-anilino-α-glucofuranose as an antitumor core structure that may open a new way to develop more potent anti-cancer agents.
Diarylamino glucosan derivative, and preparation method and anti-tumor purpose thereof
-
Paragraph 0097; 0098; 0099; 0100, (2017/04/26)
The invention belongs to the field of medicinal chemistry, and particularly relates to a diarylamino glucosan derivative, and a preparation method and an anti-tumor purpose thereof, wherein the diarylamino glucosan derivative particularly relates to a compound shown as a formula I. The invention also relates to the preparation method of the diarylamino glucosan derivative, and the purpose of the diarylamino glucosan derivative in an aspect of preparing medicine for treating tumor diseases. The diarylamino glucosan derivative particularly has the obvious inhibition effects on human skin quamous cell carcinoma cells, human lung carcinoma cells and human colon cancer cells.