96202-57-2Relevant academic research and scientific papers
Synthesis of substituted tryptanthrin via aryl halides and amines as antitumor and anti-MRSA agents
Chen, Huan,Hou, Baolong,Liu, Jianli,Liu, Li,Ma, Xiumei,Wang, Cuiling,Wang, Jilin,Wang, Rui,Wang, Yinyin,Zheng, Xudong
, (2019/11/13)
The natural alkaloid, tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione), and its analogues are found to exhibit potent antitumor and anti-MRSA activities. An efficient and convenient method has been developed for the synthesis of tryptanthrin D-ring derivatives through the reaction of substituted tryptanthrins and secondary amines in moderate to good yields. Some of the new compounds exhibited antitumor activities against the human tumor cell lines A549, HCT116 and MDA-MB-231, with mean IC50 values at low micromolar levels. In addition, some of the compounds showed excellent anti-MRSA activities and were more effective than vancomycin, with MIC values of 0.31–1.25 μg/mL for Mu50,RN4220, and Newman strains.
Utilizing Solubility differences to achieve regiocontrol in the synthesis of substituted quinoline-4-carboxylic acids
Lindsay-Scott, Peter J.,Barlow, Helen
supporting information, p. 1516 - 1520 (2016/06/14)
A practical method for the regiocontrolled synthesis of substituted quinoline-4-carboxylic acids is described. Solubility differences between the product quinoline regioisomers enable their facile separation, thus avoiding any challenging chromatographic purifications and allowing access to highly substituted quinoline compounds in three steps from commercially available anilines.
TRPV4 ANTAGONISTS
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Page/Page column 37, (2011/10/13)
The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
TRPV4 ANTAGONISTS
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Page/Page column 39, (2011/10/13)
The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
Synthesis and biophysical evaluation of arylhydrazono-1H-2-indolinones as β-amyloid aggregation inhibitors
Campagna, Francesco,Catto, Marco,Purgatorio, Rosa,Altomare, Cosimo D.,Carotti, Angelo,De Stradis, Angelo,Palazzo, Gerardo
scheme or table, p. 275 - 284 (2011/02/27)
A series of isatin-3-arylhydrazones were synthesized and evaluated in vitro as inhibitors of Aβ1-40 aggregation using a thioflavin T fluorescence method. An exploration of the effects on Aβ1-40 aggregation of a number of diverse subs
Synthesis and cytostatic evaluation of some 2-(5-substituted-2-oxoindolin- 3-ylidene)-N-substituted hydrazine carbothioamide
Karki, Subhas S.,Kulkarni, Amol,Teraiya, Nishith,Clercq, Erik De,Balzarini, Jan
scheme or table, p. 1229 - 1234 (2012/06/04)
Various substituted 2-(5-substituted-2-oxoindolin- 3-ylidene)-N-substituted hydrazine carbothioamide 4a-g and 2-(5-substituted-1-(4-substituted benzyl)-2-oxoindolin- 3-ylidene)-N-substituted hydrazine carbothioamide 5a-k were synthesized. The compounds were evaluated for their cytostatic activity against human Molt4/C8 and CEM T-lymphocytes as well as murine L1210 leukemia cells. Several of these compounds were endowed with low micromolar 50%-inhibitory concentration (IC50) values, and some were virtually equally potent as melphalan. The most potent inhibitors against the murine leukemia cells were also most inhibitory against human T-lymphocyte tumor cells. 2-(5-fluoro-1-(4-fluorobenzyl)-2-oxoindolin-3- ylidene)-N-p-tolylhydrazine carbothioamide (5b) emerged as the most potent cytostatic compound among the tested compounds. The encouraging cytostatic data provide an adequate rationale for further modification of these molecular scaffolds. Springer Science+Business Media, LLC 2010.
Synthesis and antibacterial activity of pyridazino[4,3-b]indole-4-carboxylic acids carrying different substituents at N-2
Palluotto, Fausta,Campagna, Francesco,Carotti, Angelo,Ferappi, Marcello,Rosato, Antonio,Vitali, Cesare
, p. 63 - 69 (2007/10/03)
The synthesis and the in vitro evaluation of antibacterial activity of new pyridazino[4,3-b]indole-4-carboxylic acids 2-4, 6 against some selected representative of Gram-positive and Gram-negative bacteria are reported. The role of the lipophilicity in th
