90763-46-5Relevant academic research and scientific papers
Synthesis, characterisation and metal complexation reactions of two calix[4]arene derivatives functionalised with pendant benzamide arms
McGinley, John,McKee, Vickie,Walsh, John M.D.
, p. 57 - 62 (2011)
Two calix[4]arene derivatives (3 and 4) functionalised at the lower rim with pendant benzamide arms were successfully synthesised and characterised, with the X-ray crystal structure of 3 being determined. Only 4 took part in some metal ion complexation re
Synthesis and in vitro anti-platelet aggregation activities of 2-methoxy-5-arylamido-N-(pyridin-3-yl-methyl)benzamides
Wang, Yan,Wang, Xiao,Chen, Xin,Liu, Xiujie
, (2018/12/11)
In order to discover novel compounds with anti-platelet aggregation activities, a series of novel 2-methoxy-5-arylamido-N-(pyridin-3-ylmethyl)benzamides (1a–n) were synthesized and their anti-platelet aggregation activities were evaluated by the turbidimetric method in response to the following agonists: adenosine diphosphate (ADP) (5 mM/L), arachidonic acid (AA) (20 μM/L), and collagen (1 mg/mL). Those synthesized compounds that have better in vitro activities were subjected to cell toxicity tests via cell counting kit-8 (CCK-8) assay. The biological evaluation revealed that compound 1a (IC50: 0.21 μM/L) exhibited the highest anti-platelet aggregation activities when ADP was selected as an inducer, and compound 1b (IC50: 0.23 μM/L) showed the best activities when AA was selected as inducer, and compound 1m (inhibition rate: 55.06%) had significant anti-platelet aggregation activities when collagen was selected as inducer among all target compounds. Moreover, the effect of cell toxicity exhibited that none of the compounds had obvious cell toxicity against L929 cells. Therefore, 2-methoxy-5-arylamido-N-(pyridin-3-ylmethyl)benzamides have the potential to become a novel kind of anti-platelet drugs and deserve further study.
Synthesis and evaluation of in vitro antiplatelet aggregation activities of 2-Methoxy-5-Aminobenzamides
Liu, Lili,Liu, Xiujie,Chen, Guangling,Qiu, Kai
, p. 1040 - 1050 (2019/10/28)
Objective: According to the principles of drug design, the structures of picotamide and betrixaban were combined to design novel series of 2-methoxy-5-aminobenzamides. A total of twenty new compounds 1a-1t have been synthesized and evaluated for their ant
A model β-sheet interaction and thermodynamic analysis of β-strand mimetics
Robinson, Colin W.,Rye, Carl S.,Chessum, Nicola E. A.,Jones, Keith
supporting information, p. 7402 - 7407 (2015/07/15)
β-Sheet mediated protein-protein interactions are involved in key signalling pathways in diseases such as cancer. We present small molecule β-strand mimetics and investigate their interactions with a model tripeptide. Using 1H NMR, the thermodynamic parameters for their binding are determined. These give insight into this biologically important interaction.
A model β-sheet interaction and thermodynamic analysis of β-strand mimetics
Robinson, Colin W.,Rye, Carl S.,Chessum, Nicola E. A.,Jones, Keith
supporting information, p. 7402 - 7407 (2015/11/27)
β-Sheet mediated protein-protein interactions are involved in key signalling pathways in diseases such as cancer. We present small molecule β-strand mimetics and investigate their interactions with a model tripeptide. Using 1H NMR, the thermodynamic parameters for their binding are determined. These give insight into this biologically important interaction.
Quadruply hydrogen-bonded heteroduplexes based on imide and urea units arrayed with ADDA/DAAD sequences
Li, Xianghui,Jia, Yiming,Ren, Yi,Wang, Youjia,Hu, Jinchuan,Ma, Teng,Feng, Wen,Yuan, Lihua
, p. 6975 - 6983 (2013/10/08)
A new class of imide- and urea-based hetero-strands with a quadruple ADDA/DAAD hydrogen-bond array was designed and synthesized from easily accessible starting materials. The molecular recognition between the two different strands depends highly on the su
Self-complementary quadruply hydrogen-bonded duplexes based on imide and urea units
Li, Xianghui,Fang, Yuyu,Deng, Pengchi,Hu, Jinchuan,Li, Tian,Feng, Wen,Yuan, Lihua
supporting information; experimental part, p. 4628 - 4631 (2011/11/06)
The quadruply hydrogen-bonded duplexes based on an imide-urea structure preorganized by three-center hydrogen bonds were found to associate via bifurcated hydrogen bonds. 1H NMR dilution experiments revealed the high stability of the homodimer in apolar solvent (Kdim > 10 5 M-1 in CDCl3) and enhancement of association ability due to electron-withdrawing substituent effects. The ready synthetic availability and adjustable association affinity via electronic effects may render these association units potentially applicable in constructing supramolecular architectures.
Benzoylurea derivatives as a novel class of antimitotic agents: Synthesis, anticancer activity, and structure-activity relationships
Song, Dan-Qing,Wang, Yan,Wu, Lian-Zong,Yang, Peng,Wang, Yue-Ming,Gao, Li-Mei,Li, Yan,Qu, Jing-Rong,Wang, Yong-Hong,Li, Ying-Hong,Du, Na-Na,Han, Yan-Xing,Zhang, Zhi-Ping,Jiang, Jian-Dong
experimental part, p. 3094 - 3103 (2009/04/06)
Forty-six new compounds were synthesized on the basis of our knowledge of the 3-haloacylamino benzoylurea (HBU) series. Structure-activity relationship (SAR) analysis indicates that (i) the configuration of the chiral center in 1 (JIMB01) is not indispensable for the activity, (ii) the phenyl ring is essential, and (iii) a substitution at the 6-position of the phenyl ring with a halogen enhances the activity. Among the analogues, 11e and 14b bearing 6-fluoro substitution showed potent activities against nine human tumor cell lines, including CEM (leukemia), Daudi (lymphoma), MCF-7 (breast cancer), Bel-7402 (hepatoma), DU-145 (prostate cancer), PC-3 (prostate cancer), DND-1A(melanoma), LOVO (colon cancer), and MIA Paca (pancreatic cancer) with IC50 values between 0.01 and 0.30 μM. 14b inhibited human hepatocarcinoma by 86% in volume in nude mice. The mechanism of 14b is to inhibit microtubule assembly, followed by the M-phase arrest, bcl-2 inactivation, and then apoptosis. We consider 14b promising for further anticancer investigation.
ANTIFUNGAL AGENTS
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Page/Page column 62, (2008/06/13)
Compounds of formula (I), and pharmaceutically acceptable salts thereof, may be used in therapy, for example as antifungal agents: (I) wherein: Rl, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. Certain compounds of formula (I) are also provided. Compounds of formula (T), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
Acryloylamino-salicylanilides as EGFR PTK inhibitors
Deng, Wei,Guo, Zongru,Guo, Yanshen,Feng, Zhiqiang,Jiang, Yi,Chu, Fengming
, p. 469 - 472 (2007/10/03)
A series of acryloylamino-salicylanilides were synthesized as inhibitors of EGFR PTK. A strategy of pseudo six-membered ring formed through intramolecular hydrogen bonding in salicylanilides is employed to mimic the planar pyrimidine ring of quinazoline E
