30992-63-3Relevant academic research and scientific papers
NOVEL COMPOUNDS AND THEIR USE
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Page/Page column 113-114, (2021/06/26)
The present invention provides compounds of the general formula (I) or a pharmaceutically acceptable prodrugs, salts and/or solvates thereof, wherein LHS is selected from the group consisting of LHSa and LHSb And wherein, the asterisk (*) marks the point of attachment; These compounds exhibit antibacterial activity against Gram-negative and Gram-positive bacteria, especially S. aureus, E. coli, K. pneumoniae and A. baumannii. Pharmaceutical compositions containing these compounds, therapeutic uses thereof and methods for manufacturing the same are also provided.
Copper(II)-Catalyzed Tandem Reaction: Synthesis of Furo[3,2- c]coumarin Derivatives and Evaluation for Photophysical Properties
Feng, Xi,Qin, Zhen,Cheng, Xinying,Liu, Dongyu,Peng, Yinghe,Huang, Huidan,Song, Bin,Bian, Jinlei,Li, Zhiyu
supporting information, p. 12537 - 12548 (2021/09/20)
An efficient protocol for synthesizing furo[3,2-c]coumarin derivatives is described. The novel reaction could afford the desired furocoumarins with good to excellent yields in a mild and rapid manner. Large substrate scope screening and scale-up preparation have also been accomplished, and selected compounds were evaluated for their photophysical properties.
Design, synthesis, and biological activity of a novel series of benzofuran derivatives against oestrogen receptor-dependent breast cancer cell lines
Hu, Chun,Hu, Jian-Shu,Huang, Er-Fang,Jin, Li-Ping,Jin, Zhe,Wan, David Chi-Cheong,Wang, Lin,Xie, Qian,Zhang, Bing-Qi
, (2020/01/13)
A docking study of a novel series of benzofuran derivatives with ERα was conducted. In this study, we report the synthesis of a novel series of benzofuran derivatives and evaluation of their anticancer activity in vitro against MCF-7 human breast cancer cells, as well as their potential toxicity to ER-independent MDA-MB-231 breast cancer cells, human renal epithelial HEK-293 cells, and human immortal keratinocytes (HaCaT cells) by using the MTT colorimetric assay. The screening results indicated that the target compounds exhibited anti-breast cancer activity. The target compound 2-benzoyl-3-methyl-6-[2-(morpholin-4-yl)ethoxy]benzofuran hydrochloride (4e) exhibited excellent activity against anti-oestrogen receptor-dependent breast cancer cells and low toxicity. The preliminary structure-activity relationships of the target benzofuran derivatives have been summarised. In conclusion, the novel benzofuran scaffold may be a promising lead for the development of potential oestrogen receptor inhibitors.
CLASS OF BIFUNCTIONAL COMPOUNDS WITH QUATERNARY AMMONIUM SALT STRUCTURE
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Paragraph 0168, (2019/11/11)
The invention provides a class of compounds represented by formula (I), having bifunctional active quaternary ammonium salt structure of a β2-adrenoreceptor agonist and an M receptor antagonist, a pharmaceutically acceptable salt, solvate, and optical isomer thereof. A pharmaceutical composition comprising such a compound with quaternary ammonium salt structure, a method for preparing such a compound with quaternary ammonium salt structure and an intermediate thereof, and uses thereof in treating pulmonary disorders are also provided. The compounds of the invention have high selectivity to the M receptor subtype, and have less adverse reaction and lower toxic and side effects in the treatment of pulmonary diseases such as COPD and asthma.
COMPOUNDS AND METHODS FOR INHIBITING EMT PATHWAYS TO TREAT CANCER, ORGAN FIBROSIS AND METABOLIC DISORDERS
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Page/Page column 22; 23, (2018/09/19)
A compound, or a pharmaceutically acceptable salt or isomer thereof, of Formula I: wherein R is hydrogen, alkyl, substituted alkyl, alkenyl, or substituted alkenyl; R1 is hydrogen, alkoxy, or substituted alkoxy; R2 is hydrogen, alkyl, or substituted alkyl; and R3 is hydrogen, alkyl, or substituted alkyl.
5-[2-hydroxy-3-(alkylamine) propoxy] benzofuran compound and application thereof
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Paragraph 0036; 0044; 0045, (2018/04/21)
The invention belongs to the technical field of medicines and relates to a 5-[2-hydroxy-3-(alkylamine) propoxy] benzofuran compound and the application thereof. The 5-[2-hydroxy-3-(alkylamine) propoxy] benzofuran compound comprises a stereisomer of the compound and pharmaceutically applicable salt; the general molecular formula of the compound is shown as follows: wherein R is described as the claims and the specification. The 5-[2-hydroxy-3-(alkylamine) propoxy] benzofuran compound and the pharmaceutically applicable acid addition salt of the compound can be combined with the existing drug for use or can be used alone, and are used for preparing a drug for treating a vascular smooth muscle spastic disease.
5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran derivatives and application thereof
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Paragraph 0036; 0037; 0038, (2018/06/15)
The invention belongs to the technical field of medicines, and relates to 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran derivatives and an application thereof. The 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran derivatives comprise stereoisomers and pharmaceutically acceptable salts of 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran, and the structural formula of the derivatives is shownin the description. The 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran derivatives and the pharmaceutically acceptable acid addition formed salts of 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran can be used together with existing medicines or individually, and are used for preparing medicines for treating blood vessel smooth muscle spasm diseases.
One-pot two-step synthesis of 3-iodo-4-aryloxy coumarins and their Pd/C-catalyzed annulation to coumestans
Panda, Niranjan,Mattan, Irshad
, p. 7716 - 7725 (2018/03/01)
An efficient protocol for the synthesis of various coumestans from the intramolecular annulation of 3-iodo-4-aryloxy coumarins through C-H activation has been developed. When 3-iodo-4-aryloxy coumarins were treated with 10% Pd/C (0.3 mol% Pd) in the presence of sodium acetate, the corresponding coumestans were produced in good to excellent yield. Reusability of the palladium catalyst was investigated in up to three consecutive cycles and it was found that the yield of the reaction was almost unaltered. Sequential iodination and O-arylation of 4-hydroxy coumarins leading to the 3-iodo-4-aryloxy coumarins were also achieved in a one-pot two-step process starting from aryl iodides in high yield. Pivalic acid was revealed to be the most effective additive for the later method to produce 3-iodo-4-phenoxy coumarins. Different functional groups bearing electron-donating as well as withdrawing groups are also tolerant to the reaction conditions.
Benzoxazine compound and its preparation methods and application
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Paragraph 0051; 0056; 0057, (2017/10/07)
The invention relates to a benzoxazine compound represented in the following formula 1. The benzoxazine compound can serve as a beta 2 receptor agonist. The formula can be seen from the description.
The synthesis and evaluation of flavone and isoflavone chimeras of novobiocin and derrubone
Mays, Jared R.,Hill, Stephanie A.,Moyers, Justin T.,Blagg, Brian S.J.
experimental part, p. 249 - 266 (2010/04/05)
The natural products novobiocin and derrubone have both demonstrated Hsp90 inhibition and structure-activity relationships have been established for each scaffold. Given these compounds share several key structural features, we hypothesized that incorporation of elements from each could provide insight to structural features important for Hsp90 inhibition. Thus, chimeric analogues of novobiocin and derrubone were constructed and evaluated. These studies confirmed that the functionality present at the 3-position of the isoflavone plays a critical role in determining Hsp90 inhibition and suggests that the bicyclic ring system present in both novobiocin and derrubone do not share similar modes of binding.
