865722-99-2Relevant academic research and scientific papers
Total synthesis of psammaplysenes A and B, naturally occurring inhibitors of FOXO1a nuclear export
Georgiades, Savvas N.,Clardy, Jon
, p. 4091 - 4094 (2005)
(Chemical Equation Presented) Two inhibitors of FOXO1a-mediated nuclear export, psammaplysenes A and B, have been synthesized by a flexible and efficient route. A common starting material, 4-iodophenol, was used to prepare both halves of these pseudosymme
Practical synthesis of spermine, thermospermine and norspermine
Kariya, Yuka,Asanuma, Yuta,Inai, Makoto,Asakawa, Tomohiro,Ohashi-Ito, Kyoko,Fukuda, Hiroo,Egi, Masahiro,Kan, Toshiyuki
, p. 1403 - 1407 (2016/09/09)
Polyamines, such as spermine (1), thermospermine (2) and norspermine (3), are widely distributed in nature, and have multiple biological activities. In addition, many of their conjugates have potential for pharmacological use. Here, we present a solid-phase synthesis using our nitrobenzenesulfonyl (Ns) strategy, which can provide 1, 2 and 3 on a gram scale. This approach should be suitable for facile construction of a diverse library of polyamines.
Molecular construction of HIV-gp120 discontinuous epitope mimics by assembly of cyclic peptides on an orthogonal alkyne functionalized TAC-scaffold
Werkhoven,Elwakiel,Meuleman,Quarles Van Ufford,Kruijtzer,Liskamp
, p. 701 - 710 (2016/01/12)
Mimics of discontinuous epitopes of for example bacterial or viral proteins may have considerable potential for the development of synthetic vaccines, especially if conserved epitopes can be mimicked. However, due to the structural complexity and size of discontinuous epitopes molecular construction of these mimics remains challeging. We present here a convergent route for the assembly of discontinuous epitope mimics by successive azide alkyne cycloaddition on an orthogonal alkyne functionalized scaffold. Here the synthesis of mimics of the HIV gp120 discontinuous epitope that interacts with the CD4 receptor is described. The resulting protein mimics are capable of inhibition of the gp120-CD4 interaction. The route is convergent, robust and should be applicable to other discontinuous epitopes.
Expedient synthesis of a novel asymmetric selectively deprotectable derivative of the ATAC scaffold
Brouwer, Arwin J.,Van De Langemheen, Helmus,Liskamp, Rob M.J.
, p. 4002 - 4007 (2014/06/09)
An efficient multigram scale synthesis of a new asymmetric triazacyclophane scaffold, the ATAC (Asymmetric-TAC) scaffold, bearing three selectively removable groups is described. This scaffold is slightly more rigid than our frequently used TAC (TriAzaCyc
