2028-72-0Relevant academic research and scientific papers
(E)-N-Aryl-2-oxo-2-(3,4,5-trimethoxyphenyl)acetohydrazonoyl cyanides as tubulin polymerization inhibitors: Structure-based bioisosterism design, synthesis, biological evaluation, molecular docking and in silico ADME prediction
Wang, Guangcheng,Peng, Zhiyun,Peng, Shanshan,Qiu, Jie,Li, Yongjun,Lan, Yanyu
supporting information, p. 3350 - 3355 (2018/09/12)
A series of (E)-N-Aryl-2-oxo-2-(3,4,5-trimethoxyphenyl)acetohydrazonoyl cyanides have been synthesized and evaluated for their anticancer activity in human hepatocellular liver carcinoma HepG2 and breast adenocarcinoma MCF-7 cell lines. Among all the test
Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure-Activity Relationship Study
Schiedel, Matthias,Rumpf, Tobias,Karaman, Berin,Lehotzky, Attila,Oláh, Judit,Gerhardt, Stefan,Ovádi, Judit,Sippl, Wolfgang,Einsle, Oliver,Jung, Manfred
, p. 1599 - 1612 (2016/03/05)
Sirtuins are NAD+-dependent protein deacylases that cleave off acetyl but also other acyl groups from the ε-amino group of lysines in histones and other substrate proteins. Dysregulation of human Sirt2 (hSirt2) activity has been associated with the pathogenesis of cancer, inflammation, and neurodegeneration, which makes the modulation of hSirt2 activity a promising strategy for pharmaceutical intervention. The sirtuin rearranging ligands (SirReals) have recently been discovered by us as highly potent and isotype-selective hSirt2 inhibitors. Here, we present a well-defined structure-activity relationship study, which rationalizes the unique features of the SirReals and probes the limits of modifications on this scaffold regarding inhibitor potency. Moreover, we present a crystal structure of hSirt2 in complex with an optimized SirReal derivative that exhibits an improved in vitro activity. Lastly, we show cellular hyperacetylation of the hSirt2 targeted tubulin caused by our improved lead structure.
Tetracyclic compounds from 1-oxo-1,2,3,4,5,6-hexahydrocycloocta[b]indole. Synthesis of oxazolo[4′5′:8,7]cycloocta[b]indoles
Vandana,Velumani,Prasad, K. J. Rajendra
, p. 299 - 306 (2007/10/03)
Japp-Klingmann method was used to diazotise aniline derivatives and 2-hydroxymethylenecyclooctanone 2 to obtain cyclooctan-1′,2′ -dione-1′-arylhydrazone 3 which upon acid cyclisation using kents reagent gave 1-oxo-1,2,3,4,5,6-hexahydrocycloocta[b]indole 4
Reaction of Triazene 1-Oxides: Novel Synthesis of Solid Arenediazonium Chlorides
Mohamed, Shaaban K.,Gomaa, Mohsen A.-M.,Nour El-Din, Ahmed M.
, p. 166 - 167 (2007/10/03)
Treatment of 1,3-diaryltriazene 1-oxides with oxalyl chloride in dry toluene at room temperature gives only solid arenediazonium chlorides; however, treatment with acetyl and benzoyl chlorides does not afford the corresponding diazonium chlorides.
FORMATION OF ARENEDIAZONIUM ION IN OXIDATION OF N,N-DIMETHYL-4-AMINOBENZENE AND SOME meta-SUBSTITUTED DERIVATIVES WITH CERIMU(IV) ION IN ACID MEDIUM
Matrka, Miroslav,Pipalova, Jitka
, p. 2711 - 2715 (2007/10/02)
Oxidation has been studied of an experimental hepatocarcinogene N,N-dimethyl-4-aminoazobenzene and some its meta-substituted derivatives with cerium(IV) ion in 1M hydrochloric acid medium with potentiometric indication.It has been possible to prove format
Polarography of Some Arylazothiohydantoin Derivatives
Darwish, S.,Fahmy, H. M.,Abdel Aziz, M. A.,El Maghraby, A. A.
, p. 344 - 349 (2007/10/02)
The polarographic behaviour of a series of arylazothiohydantoin derivatives has been investigated at a dropping mercury electrode.Two wawes were displayed.The first and predominant one is due to the reductive splitting of the azo-linkage by a 4e irreversi
