- Research on Crystal Structure and Fungicidal Activity of the Amide Derivatives Based on the Natural Products Sinapic Acid and Mycophenolic Acid
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Structural optimization based on natural products is an important and effective way to discover new green pesticides. Here, two series of amide derivatives based on sinapic acid and mycophenolic acid were designed in combination with the fungicidal natura
- Bazhanau, Dzmitry,Chen, Zhanfang,Chu, Pengfei,Fang, Hongbin,Hua, Xuewen,Liu, Wenrui,Liu, Yi,Ru, Jing,Wang, Bingxiang,Xue, Chenmeng,Yuan, Man,Zhu, Xiaohe
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- Design and synthesis of cenocladamide analogues and their evaluation against breast cancer cell lines
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This work describes the total synthesis of the alkaloid cenocladamide and a concise library of nine structural analogues aiming at their evaluation against the breast cancer cell line MDA-MB-231. The most promising compound (3; IC50 = 6.6 μM) was also evaluated in a panel of seven breast cancer cell lines and two non-tumorigenic cell lines. We further conducted an initial investigation on the mechanism of action of analogue 3, which lacks the endocyclic double bond when compared to cenocladamide. The present study presents the discovery of a cenocladamide analogue with interesting cytotoxic activity, which could be useful for further optimization towards new chemotherapeutic agents for breast cancer treatment.
- Santos, Carla C. F.,Paradela, Luciana S.,Novaes, Luiz F. T.,Dias, Sandra M. G.,Pastre, Julio C.
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p. 755 - 766
(2017/04/27)
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- DERIVATIVES OF THE SINAPINIC ACID
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The object of the present invention is a compound of general formula (I) as well as to its pharmaceutically acceptable salt, and to the use of this compound for cosmetic and pharmaceutical applications.
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Paragraph 0094; 0095; 0096; 0097
(2016/01/10)
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- Synthesis of hydroxyethyl starch derivatives with phenylpropanoid fragments attached through ester or sulfide bonds
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Approaches to the synthesis of hydroxyethyl starch derivatives containing phenylpropanoic acid fragments with various degree of substitution were suggested. Esterification of hydroxyethyl starch in heterogeneous aqueous organic medium gave rise to the cor
- Torlopov,Udoratina,Belyaev
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p. 2130 - 2135
(2015/06/08)
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- A newly synthesized sinapic acid derivative inhibits endothelial activation in vitro and in vivos
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Inhibition of oxidative stress and inflammation in vascular endothelial cells (ECs) may represent a new therapeutic strategy against endothelial activation. Sinapic acid (SA), a phenylpropanoid compound, is found in natural herbs and high-bran cereals and has moderate antioxidant activity. We aimed to develop new SA agents with the properties of antioxidation and blocking EC activation for possible therapy of cardiovascular disease. We designed and synthesized 10 SA derivatives according to their chemical structures. Preliminary screening of the compounds involved scavenging hydroxyl radicals and 2,2-diphenyl-1- picrylhydrazyl (DPPH×), croton oil-induced ear edema in mice, and analysis of the mRNA expression of adhesion molecules in ECs. 1- Acetyl-sinapic acyl-4-(39-chlorine-)benzylpiperazine (SA9) had the strongest antioxidant and anti-inflammatory activities both in vitro and in vivo. Thus, the effect of SA9 was further studied. SA9 inhibited tumor necrosis factor a-induced upregulation of adhesion molecules in ECs at both mRNA and protein levels, as well as the consequent monocyte adhesion to ECs. In vivo, result of face-toface immunostaining showed that SA9 reduced lipopolysaccharideinduced expression of intercellular adhesion molecule-1 in mouse aortic intima. To study the molecular mechanism, results from luciferase assay, nuclear translocation of NF-kB, and Western blot indicated that the mechanism of the anti-inflammatory effects of SA9 might be suppression of intracellular generation of ROS and inhibition of NF-kB activation in ECs. SA9 is a prototype of a novel class of antioxidant with anti-inflammatory effects in ECs. It may represent a new therapeutic approach for preventing endothelial activation in cardiovascular disorders.
- Zeng, Xiaoyun,Zheng, Jinhong,Fu, Chenglai,Su, Hang,Sun, Xiaoli,Zhang, Xuesi,Hou, Yingjian,Zhu, Yi
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p. 1099 - 1108
(2013/06/27)
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- Antioxidant potential of hydroxycinnamic acid glycoside esters
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Hydroxycinnamic acids are natural antioxidants found in fruits, vegetables, and cereals. In this study, the antioxidant activity of various types of hydroxycinnamoyl glycoside esters that mimic the structure of polymeric carbohydrates was studied in diffe
- Kylli, Petri,Nousiainen, Paula,Biely, Peter,Sipilae, Jussi,Tenkanen, Maija,Heinonen, Marina
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scheme or table
p. 4797 - 4805
(2010/03/31)
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- Thienopyridine derivatives and their pharmaceutical use
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Thienopyridine derivatives of the formula (I): STR1 wherein the ring A is an optionally substituted benzene ring; the ring B is an optionally substituted thiophene ring: X is a group of the formula: STR2 (wherein R1 is hydrogen, alkyl or alkoxy
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- Sulphite-promoted delignification of wood: identification of paucidisperse lignosulphonates
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Paucidisperse lignosulphonates, previously described as a distinct group of compounds called "hemilignins" (Mw ca. 2000), were conclusively shown to be a complex mixture of monomeric (C9) sulphonic acids.Since these compounds are rapidly solubilized only during the early stages of delignification from softwoods (/= 30percent lignin removal), it can be concluded that they are selectively removed from the secondary wall and not from the middle lamella.This result gives chemical support to the hypothesis that morphological differences in lignin stucture exist.It is proposed that the generation of monolignols and their sulphonated derivatives may occur via an α-O-aryl bond cleavage rather than β-O-aryl cleavage as previously suggested.For softwoods, several other major constituents were isolated, which may be derived from sulphonation of a β-hydroxylated form of coniferyl alcohol.
- Bialski, Alec M.,Luthe, Corinne E.,Fong, Jenny L.,Lewis, Norman G.
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p. 1336 - 1344
(2007/10/02)
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