55939-13-4Relevant articles and documents
Synthesis and study of antiproliferative, antitopoisomerase II, DNA-intercalating and DNA-damaging activities of arylnaphthalimides
Quintana-Espinoza, Patricia,Garcia-Luis, Jonay,Amesty, Angel,Martin-Rodriguez, Patricia,Lorenzo-Castrillejo, Isabel,Ravelo, Angel G.,Fernandez-Perez, Leandro,Machin, Felix,Estevez-Braun, Ana
supporting information, p. 6484 - 6495 (2013/10/22)
A series of arylnaphthalimides were designed and synthesized to overcome the dose-limiting cytotoxicity of N-acetylated metabolites arising from amonafide, the prototypical antitumour naphthalimide whose biomedical properties have been related to its ability to intercalate the DNA and poison the enzyme Topoisomerase II. Thus, these arylnaphthalimides were first evaluated for their antiproliferative activity against two tumour cell lines and for their antitopoisomerase II in vitro activities, together with their ability to intercalate the DNA in vitro and also through docking modelization. Then, the well-known DNA damage response in Saccharomyces cerevisiae was employed to critically evaluate whether these novel compounds can damage the DNA in vivo. By performing all these assays we conclude that the 5-arylsubstituted naphthalimides not only keep but also improve amonafide's biological activities.
Development and evaluation of a pharmacophore model for inhibitors of aldosterone synthase (CYP11B2)
Ulmschneider, Sarah,Negri, Matthias,Voets, Marieke,Hartmann, Rolf W.
, p. 25 - 30 (2007/10/03)
Recently, we proposed inhibition of aldosterone synthase (CYP11B2) as a novel strategy for the treatment of congestive heart failure and myocardial fibrosis and synthesized a large number of inhibitors. In this work, a pharmacophore model for CYP11B2 inhibitors was developed by superimposition of active and non-active compounds. This model was confirmed by the synthesis of two pyridyl substituted acenaphthene derivatives (A,B). This new class of compounds as well as the pharmacophore could be helpful for the discovery of novel inhibitors.
A p-benzyne to m-benzyne conversion through a 1,2-shift of a phenyl group. Completion of the benzyne cascade
Polishchuk, Alexei L.,Bartlett, Kevin L.,Friedman, Lee A.,Jones Jr., Maitland
, p. 798 - 806 (2007/10/03)
Pyrolysis of 1,6-diphenylhexa-1,5-diyne-cis-3-ene at 800-1000 °C leads to a mixture of 1- and 2-phenylbiphenylene, along with triphenylene. Formation of the two biphenylenes is taken as strong evidence of the rearrangement of a p-benzyne into a m-benzyne through a shift of one of the phenyl groups. Copyright