53732-08-4Relevant articles and documents
Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents
Zhang, Niu-niu,Liu, Zhi-yong,Liang, Jie,Tang, Yun-xiang,Qian, Lu,Gao, Ya-min,Zhang, Tian-Yu,Zhang, Tian-yu,Yan, Ming
supporting information, p. 1293 - 1304 (2018/08/28)
A series of m-amidophenol derivatives (6a-6l, 7a-7q, 9a, 9b, 12a-12c, 14 and 15) were designed and synthesized. Their antitubercular activities were evaluated in vitro against M. tuberculosis strains H37Ra and H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains. Ten compounds displayed minimal inhibitory concentrations (MICs) against M. tuberculosis H37Ra below 2.5 μg mL?1 and 6g was the most active compound (MIC = 0.625 μg mL?1). Compounds 6g and 7a also showed potent inhibitory activity against M. tuberculosis H37Rv (MIC = 0.39 μg mL?1) and several clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.39-3.125 μg mL?1). The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. They exhibited low cytotoxicity against HepG2 and RAW264.7 cell lines. The results demonstrated m-amidophenol as an attractive scaffold for the development of new antitubercular agents.
Preparation of new alkyne-modified ansamitocins by mutasynthesis
Harmrolfs, Kirsten,Mancuso, Lena,Drung, Binia,Sasse, Florenz,Kirschning, Andreas
supporting information, p. 535 - 543 (2014/04/17)
The preparation of alkyne-modified ansamitocins by mutasynthetic supplementation of Actinosynnema pretiosum mutants with alkyne-substituted aminobenzoic acids is described. This modification paved the way to introduce a thiol linker by Huisgen-type cycloaddition which can principally be utilized to create tumor targeting conjugates. In bioactivity tests, only those new ansamitocin derivatives showed strong antiproliferative activity that bear an ester side chain at C-3.
QUINAZOLINONE DERIVATIVES HAVING B-RAF INHIBITORY ACTIVITY
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Page/Page column 12, (2009/07/17)
The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.