168261-64-1Relevant academic research and scientific papers
Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors
Lopez-Tapia, Francisco,Brotherton-Pleiss, Christine,Yue, Peibin,Murakami, Heide,Costa Araujo, Ana Carolina,Reis Dos Santos, Bruna,Ichinotsubo, Erin,Rabkin, Anna,Shah, Raj,Lantz, Megan,Chen, Suzie,Tius, Marcus A.,Turkson, James
supporting information, p. 250 - 255 (2018/03/21)
The molecular determinants for the activities of the reported benzoic acid (SH4-54), salicylic acid (BP-1-102), and benzohydroxamic acid (SH5-07)-based STAT3 inhibitors were investigated to design optimized analogues. All three leads are based on an N-met
2-ARYLSULFONAMIDO-N-ARYLACETAMIDE DERIVATIZED STAT3 INHIBITORS
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Paragraph 00301, (2018/08/20)
The present disclosure provides pharmaceutical compositions comprising 2-arylsulfonamido-N-arylacetamide derivatized Stat3 inhibitors and certain pharmaceutically acceptable salts thereof, and methods of their use.
Targeting ketone drugs towards transport by the intestinal peptide transporter, PepT1
Foley, David,Bailey, Patrick,Pieri, Myrtani,Meredith, David
supporting information; scheme or table, p. 1064 - 1067 (2009/05/30)
Thiodipeptide prodrugs of the ketone nabumetone are shown to have affinity for, and be transported by, PepT1 in vitro. The Royal Society of Chemistry 2009.
The in vitro transport of model thiodipeptide prodrugs designed to target the intestinal oligopeptide transporter, PepT1
Foley, David,Pieri, Myrtani,Pettecrew, Rachel,Price, Richard,Miles, Stephen,Lam, Ho Kam,Bailey, Patrick,Meredith, David
supporting information; experimental part, p. 3652 - 3656 (2009/10/23)
A thiodipeptide carrier system is shown to be effective at enabling a range of covalently bound molecules, including benzyl, benzoyl and ibuprofen conjugates, to be transported via the intestinal peptide transporter PepT1, demonstrating its potential as a rational drug delivery target.
A convenient preparation of several N-linked glycoamino acid building blocks for efficient solid-phase synthesis of glycopeptides
Van Ameijde, Jeroen,Albada, H. Bauke,Liskamp, Rob M.J.
, p. 1042 - 1049 (2007/10/03)
A high yielding route for the preparation of several Boc- and Fmoc-protected N-linked glycopeptide monomers was presented. It was found that these building blocks can be used for the solid-phase synthesis of glycopeptides or glycopeptidomimetics. A number of short glycopeptides- collagen mimics was prepared to demonstrate this applicability. The protocol employed was expected to be suitable for the synthesis of any desired N-linked glycopeptide.
Novel ester linked glycosyl amino acids: Convenient building blocks for the synthesis of glycopeptide libraries
Tennant-Eyles, Richard J.,Fairbanks, Antony J.
, p. 391 - 401 (2007/10/03)
The completely orthogonally protected aspartic acid derivative FmocAsp(OBn)O'Bu is readily synthesized on a large scale. Deprotection of the β-carboxylic acid allows coupling to various sugar derivatives via free hydroxyl groups to produce novel glycosyl amino acids. Subsequent deprotection of either the α-acid or nitrogen is achieved cleanly to allow elaboration into an oligopeptide, whilst selective deprotection of PMB protected sugar hydroxyls is also readily achievable. Such novel glycosyl amino acid building blocks may be useful for the combinatorial synthesis of novel glycopeptide libraries.
