The present invention provides novel benzodiazepine derivatives of Formula I or pharmaceutically acceptable derivatives, polymorphs, salts or prodrugs thereof. Said compounds have potential as bromodomain (BRD) inhibitors.
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Page/Page column 86-87
(2017/02/28)
Synthesis of a biologically active triazole-containing analogue of cystatin A through successive peptidomimetic alkyne-azide ligations
"Click" protein: CuI-catalyzed cycloaddition of azides and terminal alkynes has been applied to the successive ligations of three unprotected peptide fragments. Peptidomimetic triazole ligation (PTL, see scheme) as a new method for the chemical production of bioactive proteins is applied for the synthesis of a triazole-containing analogue of the 97 amino acid protein cystatin A. Copyright
Valverde, Ibai E.,Lecaille, Fabien,Lalmanach, Gilles,Aucagne, Vincent,Delmas, Agnes F.
supporting information; experimental part
p. 718 - 722
(2012/03/10)
Solid-phase Staudinger ligation from a novel core-shell-type resin: A tool for facile condensation of small peptide fragments
Solid-phase Staudinger ligation of small peptides was performed on a novel core-shell-type resin. Solid-phase Staudinger ligation was mediated by synthetic solid-supported phosphinothiol, which was readily prepared by a straightforward synthetic route. This protocol afforded final peptide products in excellent yields and purities and thus could provide the opportunity to facilitate a simple manipulation for condensation of peptide fragments. In particular, the resulting resin could be recycled in a successful manner.
Kim, Hanyoung,Cho, Jin Ku,Aimoto, Saburo,Lee, Yoon-Sik
[structure: see text]. Pure alpha-azido acids were prepared using an efficient diazo transfer method followed by buffered workup. These building blocks were used to prepare small peptides on Wang resin by two approaches. Peptides prone to diketopiperazine formation were prepared in good yields by coupling acids to resin bound iminophosphoranes during Fmoc-Wang synthesis. The iminophosphoranes can also be hydrolyzed under neutral conditions to provide unprotected amines ready for further coupling.
Lundquist 4th.,Pelletier
p. 781 - 783
(2007/10/03)
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