6307-82-0Relevant academic research and scientific papers
Development of 2-Morpholino-N-hydroxybenzamides as anti-proliferative PC-PLC inhibitors
Rees, Shaun W.P.,Leung, Euphemia,Reynisson, Jóhannes,Barker, David,Pilkington, Lisa I.
, (2021/07/21)
Phosphatidylcholine-specific phospholipase C (PC-PLC) is a key enzyme involved in the metabolism of the mammalian phospholipid phosphatidylcholine into secondary messengers diacylglycerol (DAG) and phosphocholine. DAG and phosphocholine have been identifi
Incorporation of a nitric oxide donating motif into novel pc-plc inhibitors provides enhanced anti-proliferative activity
Rees, Shaun W. P.,Rees, Tayla A.,Leung, Euphemia,Walker, Christopher S.,Barker, David,Pilkington, Lisa I.
, (2021/10/30)
Inhibition of phosphatidylcholine-specific phospholipase C (PC-PLC) has previously been shown to be a potential target for novel cancer therapeutics. One downstream consequence of PC-PLC activity is the activation of NF-κB, a nuclear transcription factor
Development, synthesis and biological investigation of a novel class of potent PC-PLC inhibitors
Barker, David,Langley, Ries J.,Leung, Euphemia,Leung, Ivanhoe K. H.,Paulin, Emily K.,Pilkington, Lisa I.,Rees, Shaun W. P.,Reynisson, Jóhannes,Sparrow, Kevin,Xu, Chris Sun,van Rensburg, Michelle
, (2020/02/27)
Phospholipases are enzymes that are involved in the hydrolysis of acyl and phosphate esters of phospholipids, generating secondary messengers that have implications in various cellular processes including proliferation, differentiation and motility. As such inhibitors of phospholipases have been widely studied for their use as anti-cancer therapeutics. Phosphatidylcholine-specific phospholipase C (PC-PLC) is implicated in the progression of a number of cancer cell lines including aggressing triple-negative breast cancers. Most current studies on PC-PLC have utilised D609 as the standard inhibitor however it is known to have multiple failings, including poor stability in aqueous media. 2-Morpholinobenzoic acids were recently identified using vHTS as a potential class of lead compounds, with improvements over D609. In this work 129 analogues in this class were prepared and their PC-PLC inhibitory activity was assessed. It was found that the majority of these novel compounds had improved activity when compared to D609 with the most potent inhibitors completely inhibiting enzyme activity. It was determined that the best compound/s contained a morpholino and 2-substituted N-benzyl moieties with these findings explained using molecular modelling. The compounds reported here will allow for improved study of PC-PLC activity.
Aryl bithiazole compound and application
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Paragraph 0033; 0034, (2019/01/06)
The invention discloses an aryl bithiazole compound and application. A series of aryl bithiazole compounds are prepared in the invention, and application of the compounds is researched. According to biological activity test results, the aryl bithiazole compound provided by the invention has excellent herbicidal activity, has wide herbicide controlling spectrum to wheat, sorghum, barnyard grass, cucumber, oilseed rapes and radish, has a high inhibition rate on broadleaf weeds, and particularly has obvious inhibitory effects on amaranthus retroflexus and eclipta prostrate.
FORMIMIDAMIDINE COMPOUNDS USEFUL AGAINST PHYTOPATHOGENIC MICROORGANISMS
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Page/Page column 77-78, (2018/12/12)
The present invention relates to 4-substituted amidine derivatives of the general formula (I), wherein A1-A4, D, L, Q, R7, R7' and integer's v and w have the meanings as defined in description. The invention further relates to methods for their preparation and use of said compounds to fight undesired phytopathogenic microorganisms, and agents for said purpose, comprising said amidine derivatives, all according to the invention. This invention further relates to a method for controlling undesired phytopathogenic microorganisms by application of said 4-substituted amidine derivatives of general formula (I) to such undesired microorganisms and/or to their habitat, according to the invention. (I)
Acylhydrazone compounds with anti-tumor activity as well as preparation method and application of acylhydrazone compounds
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Paragraph 0039; 0040; 0041; 0042, (2018/05/16)
The invention belongs to the technical field of medicinal chemistry, and in particular relates to acylhydrazone compounds with anti-tumor activity as well as a preparation method and application of the acylhydrazone compounds. The structures of the acylhydrazone compounds are as shown in a general formula (I) shown in the description, wherein R and R' are independently selected from any one or more of halogen, amino, cyano, alkoxy, 3,4-methylenedioxy, nitro, phenyl or substituted phenyl, and R and R' substituents are mono-substituted, disubstituted or tri-substituted. The preparation method issimple; biological activity test results of the compounds show that the compounds have a very good inhibitory effect on histone methyltransferase SET7, and have good application prospect in the development of anti-tumor aspects.
Dinuclear MoV Complexes with Thiophenolate-oxazoline Ligands: Synthesis, Characterization, and Exceptional Activity in Catalytic Olefin Epoxidation
Peschel, Lydia M.,Belaj, Ferdinand,Schachner, J?rg A.,M?sch-Zanetti, Nadia C.
, p. 2808 - 2817 (2017/06/13)
The synthesis, characterization, and epoxidation catalysis of two neutral, dinuclear molybdenum(V) complexes [{MoO(Lx)(μ-O)}2] (x = 1: 1; x = 2: 2) bearing S,N-bidentate thiophenolate-oxazoline ligands (L1, L2) are described. Both complexes are
NOVEL COMPOUNDS AS CHLORIDE CHANNEL BLOCKING AGENT
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Paragraph 0365; 0366; 0367; 0368; 0369, (2015/06/03)
Disclosed is a novel compound to function as a calcium-dependent chloride channel blocking agent.
PREPARATION AND METHODS OF USE FOR ORTHO-ARYL 5- MEMBERED HETEROARYL-CARBOXAMIDE CONTAINING MULTI-TARGETED KINASE INHIBITORS
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Page/Page column 90, (2013/03/26)
The present disclosure relates to compounds of the Formula (I): and pharmaceutically acceptable salts, as kinase modulators, compatible with the Type-II inhibition of kinases.
Mechanistic insights into a copper-disulfide interaction in oxidation of imines by disulfides
Srogl, Jiri,Hyvl, Jakub,Revesz, Agnes,Schroeder, Detlef
supporting information; experimental part, p. 3463 - 3465 (2009/12/26)
The concept of using disulfides as an oxidant for Cu(i) is introduced as part of a Cu-catalyzed process leading to the formation of benzothiazole from an iminodisulfide under an inert atmosphere.
