- Sequence-defined vinyl sulfonamide click nucleic acids (VS-CNAs) and their assembly into dynamically responsive materials
-
Synthetic DNA analogues are of great interest for their application in information storage, therapeutics, and nanostructured materials, yet are often limited in scalability. Vinyl sulfonamide click nucleic acids (VS-CNAs) have been developed to overcome t
- Bischoff, Derek J.,Kloxin, April M.,Kloxin, Christopher J.,LeValley, Paige J.,Sutherland, Bryan P.
-
supporting information
p. 11263 - 11266
(2020/10/06)
-
- A Peptide Backbone Stapling Strategy Enabled by the Multicomponent Incorporation of Amide N-Substituents
-
The multicomponent backbone N-modification of peptides on solid-phase is presented as a powerful and general method to enable peptide stapling at the backbone instead of the side chains. This work shows that a variety of functionalized N-substituents suitable for backbone stapling can be readily introduced by means of on-resin Ugi multicomponent reactions conducted during solid-phase peptide synthesis. Diverse macrocyclization chemistries were implemented with such backbone N-substituents, including the ring-closing metathesis, lactamization, and thiol alkylation. The backbone N-modification method was also applied to the synthesis of α-helical peptides by linking N-substituents to the peptide N-terminus, thus featuring hydrogen-bond surrogate structures. Overall, the strategy proves useful for peptide backbone macrocyclization approaches that show promise in peptide drug discovery.
- Ricardo, Manuel G.,Marrrero, Javiel F.,Valdés, Oscar,Rivera, Daniel G.,Wessjohann, Ludger A.
-
supporting information
p. 769 - 774
(2019/01/04)
-
- COMPOUND HAVING RADIOACTIVE TECHNETIUM BINDING SITE, AND RADIOACTIVE TECHNETIUM COMPLEX THEREOF
-
PROBLEM TO BE SOLVED: To provide a radioactive technetium complex which enables a hypoxia area in a living body to be visualized. SOLUTION: The present invention provides a compound represented by a predetermined structural formula and having a radioactive technetium binding site, or salt thereof, a radioactive technetium complex thereof, a radioactive pharmaceutical composition comprising the same, and a kit used for the preparation of the same. COPYRIGHT: (C)2015,JPO&INPIT
- -
-
Paragraph 0077; 0081
(2016/10/10)
-
- Orthogonal protection of peptides and peptoids for cyclization by the thiol-ene reaction and conjugation
-
Cyclic peptides and peptoids were prepared using the thiol-ene Michael-type reaction. The linear precursors were provided with additional functional groups allowing for subsequent conjugation: an orthogonally protected thiol, a protected maleimide, or an alkyne. The functional group for conjugation was placed either within the cycle or in an external position. The click reactions employed for conjugation with suitably derivatized nucleoside or oligonucleotides were either cycloadditions (Diels-Alder, Cu(I)-catalyzed azide-alkyne) or the same Michael-type reaction as for cyclization.
- Elduque, Xavier,Pedroso, Enrique,Grandas, Anna
-
p. 2843 - 2853
(2014/05/06)
-
- Reversible α-helix formation controlled by a hydrogen bond surrogate
-
Strategically placed covalent linkages have been shown to stabilize helical conformations in short peptide sequences. Here we report the synthesis of a stabilized α-helix that utilizes an internal disulfide linkage. Structural analysis indicates that the
- Miller, Stephen E.,Kallenbach, Neville R.,Arora, Paramjit S.
-
experimental part
p. 4434 - 4437
(2012/08/08)
-
- "Turn-on" FRET-based luminescent iridium(iii) probes for the detection of cysteine and homocysteine
-
"Turn-on" FRET-based luminescent probes containing iridium(iii) complexes for the detection of Cys and Hcy have been designed and synthesized. The relationship between the steric bulk of the probe and the corresponding emission intensity enhancement towards detection of Cys and Hcy has been studied.
- Shiu, Hoi-Yan,Wong, Man-Kin,Che, Chi-Ming
-
supporting information; scheme or table
p. 4367 - 4369
(2011/06/20)
-
- Efficient solid-phase synthesis of FK228 analogues as potent antitumoral agents
-
Novel structural analogues of a HDAC inhibitor FK228 have been synthesized by modifying the most synthetically challenging unit, (3S,4E)-3-hydroxy-7- mercaptoheptenoic acid, with simple isosteric substitutions. These changes did not alter the backbone structure from FK228 but enabled facile and rapid synthesis by using readily available starting materials and high-yielding reactions. FK228 analogues were examined for their antitumoral activity on a variety of human cancer cells and led to the identification of new potent compounds.
- Di Maro, Salvatore,Pong, Rey-Chen,Hsieh, Jer-Tsong,Ahn, Jung-Mo
-
supporting information; experimental part
p. 6639 - 6641
(2009/10/17)
-
- Efficient method for the synthesis of bisaminoethanethiols and their pyrrole conjugates
-
By following the protection and deprotection approach, an efficient method for the preparation of bisaminoethanethiol ligands (N2S2) is discussed. In our attempts to synthesize certain nonpeptide analogs of neurotensin, moldel studies were performed by using these ligands for preparing the corresponding pyrrole based conjugates. This methodology provides an alternate approach for developing various target specific agents that cross the blood brain barrier.
- Li, Guolin,Ma, Qinggago,Ma, Bing,Grossman, Zachary D.,Pandey, Ravindra K.
-
p. 2849 - 2854
(2007/10/03)
-