- Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors
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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
- 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
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supporting information
p. 250 - 255
(2018/03/21)
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- 2-ARYLSULFONAMIDO-N-ARYLACETAMIDE DERIVATIZED STAT3 INHIBITORS
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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.
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Paragraph 00252
(2018/08/20)
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- PRODRUGS OF GUANFACINE
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Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.
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Page/Page column 25
(2011/04/18)
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- The in vitro transport of model thiodipeptide prodrugs designed to target the intestinal oligopeptide transporter, PepT1
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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.
- Foley, David,Pieri, Myrtani,Pettecrew, Rachel,Price, Richard,Miles, Stephen,Lam, Ho Kam,Bailey, Patrick,Meredith, David
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supporting information; experimental part
p. 3652 - 3656
(2009/10/23)
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- Synthetic studies towards diazepanone scaffolds
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The synthesis of new enantiopure polyfunctionalised diazepanone scaffolds is described. The key steps involve the opening of an azido-epoxide C4 building block derived from l-ascorbic or d-isoascorbic acid by a l-serine derivative followed by a lactonisation-lactamisation two-step sequence.
- Monasson, Olivier,Ginisty, Maryon,Mravljak, Janez,Bertho, Gildas,Gravier-Pelletier, Christine,Le Merrer, Yves
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body text
p. 2320 - 2330
(2010/03/25)
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- Efficient synthesis of polyfunctionalised enantiopure diazepanone scaffolds
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The synthesis of polyfunctionalised enantiopure 1,4-diazepan-3-one scaffolds from l-serine derivatives and azidoepoxides readily available from either l-ascorbic or d-isoascorbic acid, allowing access to various configurations at chiral centres, is descri
- Monasson, Olivier,Ginisty, Maryon,Bertho, Gildas,Gravier-Pelletier, Christine,Le Merrer, Yves
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p. 8149 - 8152
(2008/03/13)
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- Introduction of the Aib-Pro unit into peptides by means of the 'azirine/oxazolone method' on solid phase
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A method for the direct introduction of Aib-Pro into peptides on solid phase was developed. The Aib-Pro unit was introduced by means of the 'azirine/oxazolone method' using allyl N-(2,2-dimethyl-2H-azirin-3-yl)-l-prolinate as the synthon. After the reacti
- Stamm, Simon,Heimgartner, Heinz
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p. 9671 - 9680
(2007/10/03)
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- 3-SUBSTITUTED β-LACTAMYL VASOPRESSIN V1A ANTAGONISTS
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Novel 2-(azetidin-2-on-1-yl)alkanedioic acids and derivatives thereof are described. Methods for using 2-(azetidin-2-on-l-yl)alkanedioic acids and derivatives thereof in the treatment of disease states responsive to antagonism of the vasopressin V1a
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Page/Page column 44
(2008/06/13)
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- Access to any site-directed isotopomer of methionine, selenomethionine, cysteine, and selenocysteine - Use of simple, efficient modular synthetic reaction schemes for isotope incorporation
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Simple modular reaction schemes that allow access to any isotopomer of protected serine and homoserine have been worked out. These systems could be simply converted into cysteine, selenocysteine, homocysteine, homoselenocysteine, the essential amino acid methionine, and selenomethionine by Mitsunobu chemistry. These sulfur- and selenium-containing amino acids fulfil many essential roles in the living organism. In addition, homoserine could be converted in a few steps into optically active L-vinylglycine. As well as the stable isotopes 13C, 15N, 17O, and 18O, the radioactive isotopes of sulfur, selenium and carbon can also be easily introduced in a site-directed fashion. In view of the wide scope of the Mitsunobu reaction, we feel that many more important systems with the carbon skeleton of serine and homoserine should be preparable through this basic chemistry in any site-directed isotopically labeled form. Wiley-VCH Verlag GmbH & Co, KGaA, 69451 Weinheim, Germany, 2004.
- Siebum, Arjan H. G.,Woo, Wei Sein,Raap, Jan,Lugtenburg, Johan
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p. 2905 - 2913
(2007/10/03)
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- Selective nitrolytic deprotection of N-BOC-amines and N-BOC-amino acids derivatives
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The extension of the deprotection procedure using HNO3 in CH2Cl2 to a number of appropriately selected N-BOC-masked amines and derivatives of natural amino acids was investigated. The method was found to work effectively with almost all tested substrates, with the exception of activated aromatic amines and heterocycles which underwent unavoidable faster oxidation. Alanine, phenylalanine, serine and lysine derivatives were efficiently deprotected, as well as dipeptide Ala-Phe, preserving the configuration of the substrates and without affecting copresent Z and ester functions, with a remarkable selectivity towards acid sensitive t-butyl esters. The obtained amino acids esters, isolated and characterized in the form of nitrates salts, proved to be suitable intermediates to be used in peptide synthesis.
- Strazzolini, Paolo,Melloni, Tiziana,Giumanini, Angelo G
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p. 9033 - 9043
(2007/10/03)
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- Synthesis of β-lactams via ring opening of a serine derived aziridine
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Serine derived aziridine 15 was successfully ring-opened with amino acid esters to give diaminopropionic acid derivatives in excellent yield and regioselectivity. These compounds were cyclised to form the corresponding β-lactams in good overall yield. One
- Turner,Sikkema,Filippov,Van der Marel,Van Boom
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p. 1727 - 1730
(2007/10/03)
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- Chelating compounds, their chelates with paramagnetic metal ions, their preparation and use
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Compounds which can chelate paramagnetic bi- and trivalent metal ions, their chelates with said metal ions and their use as contrast agents in magnetic resonance imaging (MRI), the compounds having formula (I) wherein Ris a -(CH2)m-O
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