6238-12-6Relevant articles and documents
Synthesis and antileishmanial evaluation of thiazole orange analogs
Abdelhameed, Ahmed,Liao, Xiaoping,McElroy, Craig A.,Joice, April C.,Rakotondraibe, Liva,Li, Junan,Slebodnick, Carla,Guo, Pu,Wilson, W. David,Werbovetz, Karl A.
supporting information, (2019/11/28)
Cyanine compounds have previously shown excellent in vitro and promising in vivo antileishmanial efficacy, but the potential toxicity of these agents is a concern. A series of 22 analogs of thiazole orange ((Z)-1-methyl-4-((3-methylbenzo[d]thiazol-2(3H)-ylidene)methyl)quinolin-1-ium salt), a commercial cyanine dye with antileishmanial activity, were synthesized in an effort to increase the selectivity of such compounds while maintaining efficacy. Cyanines possessing substitutions on the quinolinium ring system displayed potency against Leishmania donovani axenic amastigotes that differed little from the parent compound (IC50 12–42 nM), while ring disjunction analogs were both less potent and less toxic. Changes in DNA melting temperature were modest when synthetic oligonucleotides were incubated with selected analogs (ΔTm ≤ 5 °C), with ring disjunction analogs showing the least effect on this parameter. Despite the high antileishmanial potency of the target compounds, their toxicity and relatively flat SAR suggests that further information regarding the target(s) of these molecules is needed to aid their development as antileishmanials.
Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies
Gemma, Sandra,Savini, Luisa,Altarelli, Maria,Tripaldi, Pierangela,Chiasserini, Luisa,Coccone, Salvatore Sanna,Kumar, Vinod,Camodeca, Caterina,Campiani, Giuseppe,Novellino, Ettore,Clarizio, Sandra,Delogu, Giovanni,Butini, Stefania
scheme or table, p. 6063 - 6072 (2009/12/09)
A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25 μg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results.
Novel cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
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Page 105, (2010/02/09)
The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.