55943-73-2Relevant academic research and scientific papers
Synthesis of an enlarged library of dynamic DNA activators with oxime, disulfide and hydrazone bridges
Montenegro, Javier,Bang, Eun-Kyoung,Sakai, Naomi,Matile, Stefan
supporting information; experimental part, p. 10436 - 10443 (2012/10/18)
Dynamic amphiphiles have a bridge between their charged head and their hydrophobic tails. The presence of dynamic covalent bonds is of interest for differential and biosensing applications as well as for rapid access to the libraries needed to screen for gene delivery or cellular uptake of siRNA. However, efforts to develop libraries have so far concentrated on hydrazone bridges to monocationic heads. Here, we report synthesis efforts to enlarge this focused library with oxime and disulfide bridges and dynamic amphiphiles with more than one positive charge. Evaluation in fluorogenic vesicles reveals best activation of DNA as ion transporters by dynamic amphiphiles with dendritic scaffolds, doubly charged heads and four tails. Moreover, oximes, contrary to hydrazones, remain active under acidic conditions. Linear elongation of dendritic head-groups seems to cause increasing detergent effects and should therefore be avoided. Head on: Design, synthesis and evaluation of dynamic amphiphiles with singly or doubly charged peptide dendrons as head-groups; hydrazones, oximes and disulfides as bridges; and with fragrant tails are reported. Amphiphiles with two charges and four tails (see figure) are identified as the most powerful activators of DNA as ion transporters and thus as the most promising family to screen for gene and siRNA delivery. Copyright
Vitronectin receptor antagonist pharmaceuticals
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, (2008/06/13)
The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.
