72621-26-2Relevant academic research and scientific papers
Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease
Sang, Zhipei,Wang, Keren,Zhang, Pengfei,Shi, Jian,Liu, Wenmin,Tan, Zhenghuai
, p. 238 - 252 (2019/07/17)
A series of novel chalcone derivatives was designed, synthesized and evaluated as multifunctional agents for the treatment of AD. Among of these synthesized compounds, compound TM-2 was a selective BuChE inhibitor (IC50 = 2.6 μM) and selective
NSAIDs DERIVATIVES AND USES THEREOF
-
Page/Page column 31-32, (2014/08/20)
The present invention discloses novel compounds derived from NSAIDs and pharmaceutically acceptable salts thereof. Other aspects of the invention relate to use of the NSAID derivatives in treating inflammatory diseases and pharmaceutical compositions ther
Synthesis of thiophene and NO-curcuminoids for antiinflammatory and anti-cancer activities
Ahmed, Mahera M.,Khan, M. Akram,Rainsford, Kim Drummond
, p. 1483 - 1501 (2013/04/23)
In search of better NSAIDs four novel nitric oxide donating derivatives of curcumin (compounds 9a-d), and four thiophene curcuminoids (compounds 10a-c, 11) have been synthesised. The cytotoxic effects of these compounds along with the lead compound curcumin (7) and their effect on the production of the reactive oxygen species nitric oxide and pro-inflammatory cytokines IL-1β, TNF-α and chemokine CXCL-8 were evaluated using human monocytic THP-1 and colon adenocarcinoma CACO-2 cell lines. All of the nitric oxide donating curcuminoids 9a-d and the thiophene curcuminoids 10a-c and 11 were non-cytotoxic to THP-1 cells over a concentration range of 10-100 μM and compared with curcumin compounds 10b and 10c, were more toxic. In CACO-2 cells, 10b and 11 appeared to be non-toxic at 10 to 50 μM, whereas 10a and 10c were non-cytotoxic at 10 μM only. These results clearly indicate that the introduction of a nitroxybutyl moiety to curcumin and replacement of phenyl rings with thiophene units reduces the cytotoxic effect of the parent curcumin, whereas a methyl substituted thiophene increases the cytotoxic effects. In THP-1 cells, drugs 10a and 11 significantly decreased IL-1-β production at their non-cytotoxic concentrations, whereas, they did not decrease TNF-α production in CACO-2 cells. Compound 11 showed a significant decrease in CXCL-8 production.
Synthesis and biological evaluation of nitric oxide releasing derivatives of 6-amino-3-n-butylphthalide as potential antiplatelet agents
Wang, Xiaoli,Wang, Linna,Huang, Zhangjian,Sheng, Xiao,Li, Tingting,Ji, Hui,Xu, Jinyi,Zhang, Yihua
, p. 1985 - 1988 (2013/05/09)
A series of novel nitric oxide releasing derivatives of 6-amino-3-n-butylphthalide were designed, synthesized and evaluated as potential antiplatelet agents. Compound 10b significantly inhibited the adenosine diphosphate (ADP)-induced platelet aggregation
Hybrid angiogenesis inhibitors: Synthesis and biological evaluation of bifunctional compounds based on 1-deoxynojirimycin and aryl-1,2,3-triazoles
Zhou, Ying,Zhao, Yunxue,O' Boyle, Kathy M.,Murphy, Paul V.
, p. 954 - 958 (2008/09/20)
Synthesis of hybrids of 1-deoxynojirimycin (DNJ) and 5-aryl-1,2,3-triazole as potential bifunctional inhibitors of angiogenesis is described. The DNJ component inhibits the biosynthesis of cell surface oligosaccharides necessary for angiogenesis, whereas the aryl-1,2,3-triazole inhibits methionine aminopeptidase II, a target in angiogenesis therapy. One bifunctional compound was a more potent inhibitor of angiogenesis in vitro than DNJ alone or the 5-aryl-1,2,3-triazole alone.
Hybrids of 1-deoxynojirimycin and aryl-1,2,3-triazoles and biological studies related to angiogenesis
Zhao, Yunxue,Zhou, Ying,O'Boyle, Kathy M.,Murphy, Paul V.
, p. 6333 - 6337 (2008/12/21)
Hybrids of 1-deoxynojirimycin (DNJ) and aryl-1,2,3-triazole have been synthesized with a view to identifying an inhibitor of both α-glucosidase and methionine aminopeptidase 2 (MetAP2). One compound was a potent inhibitor of α-glucosidase at both the enzyme and cellular level, and this agent also inhibited bovine aortic endothelial cell (BAEC) growth and tube formation. The anti-proliferative activity of this hybrid is due to its ability to induce cell-cycle arrest in the G1phase. The novel agent caused a reduction in the expression of cyclin D1 but did not promote apoptosis or inhibit the phosphorylation of ERK1/2. These observations indicate that its mechanism of action is distinct from fumagillin and its analogues, which inhibit MetAP2. Stress-fibre assembly in BAECs was abolished by the novel agent indicating that the inhibition of BAEC tube formation observed is partially a result of a reduction in cell motility.
Synthesis and photophysical properties of porphyrins containing viologen units for ultrafast molecular photonics
Laudien, Robert,Yoshida, Iori,Nagamura, Toshihiko
, p. 1772 - 1777 (2007/10/03)
Several 5,15-diarylporphyrin derivatives containing viologen units as an electron acceptor for ultrafast intramolecular electron transfer have been synthesized. The fluorescence of the porphyrin-viologen linked systems was appreciably quenched by the attached viologens. In accordance with this, the formation of a charge-separated state was observed upon excitation with a femtosecond (fs) laser at 400 nm. The rate of electron transfer and back transfer was controlled by the different length of alkyl chain spacers between porphyrin and viologen. Attempts to use these porphyrin molecules as a thin film component of ultrafast parallel data processing by guided wave mode geometry were limited by gradual deterioration upon repeated fs laser excitation.
α-Cyanocinnamide derivatives: A new family of non-peptide, non-sulfhydryl inhibitors of ras farnesylation
Poradosu, Enrique,Gazit, Aviv,Reuveni, Hadas,Levitzki, Alexander
, p. 1727 - 1736 (2007/10/03)
Farnesylation of Ras and other proteins is required for their membrane attachment and normal function. Here we report on the synthesis of α-cyanocinnamide derivatives, a new family of farnesyltransferase inhibitors. These compounds are nonpeptidic and do not contain sulfhydryl groups. The most potent compound is a pure competitive inhibitor with respect to the Ras protein and mixed competitive with respect to farnesyl diphosphate. Selectivity studies against geranylgeranyltransferase and biological activities of selected compounds are described. Copyright (C) 1999.
Face to face porphyrins as synthetic host molecules
Danks, Ian P.,Lane, Trevor G.,Sutherland, Ian O.,Yap, Maurice
, p. 7679 - 7688 (2007/10/02)
The bis-zincporphyrins 9 and 11 were prepared from the bis-(3′-hydroxyphenyl)-porphyrin 6. Both bis-zincporphyrins formed complexes in CHCl3 with a variety of amines and showed a strong preference for diamines, such as H2N(CH2)nNH2 and 4,4′-dipyridyl. The limited degree of chain length recognition for the diamine guests by both hosts is associated with conformational flexibility of both host and guest but the rigid guest, 4,4′-dipyridyl, is selectively complexed through operation of the chelate effect.
