108288-15-9Relevant articles and documents
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)
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.
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.
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