171905-37-6Relevant articles and documents
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
-
Paragraph 00462, (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.
ANTIBACTERIAL COMPOUNDS
-
Page/Page column 177, (2017/04/11)
This invention relates to antibacterial and antimycobacterial drug compounds of formula (I). It also relates to pharmaceutical formulations of antibacterial drug compounds of formula (I). It also relates to uses of the derivatives in treating bacterial infections and to methods of treating bacterial infections. The compounds are particularly useful for treating bacterial infections that have developed resistance to other drug compounds, e.g. resistant strains of S. aureus.
Homochiral versus Heterochiral Trifluoromethylated Pseudoproline Containing Dipeptides: A Powerful Tool to Switch the Prolyl-Amide Bond Conformation
Chaume, Grégory,Simon, Julien,Lensen, Nathalie,Pytkowicz, Julien,Brigaud, Thierry,Miclet, Emeric
, p. 13602 - 13608 (2017/12/26)
The design of constrained peptides is of prime importance in the development of bioactive compounds and for applications in supramolecular chemistry. Due to its nature, the peptide bond undergoes a spontaneous cis-trans isomerism, and the cis isomers are much more difficult to stabilize than the trans forms. By using oxazolidine-based pseudoprolines (ψPro) substituted by a trifluoromethyl group, we show that the cis peptide bond can be readily switched from 0% to 100% in Xaa-ψPro dipeptides. Our results prove that changing the configuration of the Cα in Xaa or in ψPro is sufficient to invert the cis:trans populations while changing the nature of the Xaa side chain finely tuned the conformers ratio. Moreover, a strong correlation is found between the puckering of the oxazolidine ring and the peptide bond conformation. This finding highlights the role of the trifluoromethyl group in the stabilization of the peptide bond geometry. We anticipate that such templates will be very useful to constrain the backbone geometry of longer peptides.
NOVEL ARYL-CYANOGUANIDINE COMPOUNDS
-
Page/Page column 80, (2016/10/31)
The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine- pyrazolines of general formula (I), wherein R1, R2, R3, R4 and R5 have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyperproliferative disorders, in particular for cancer, respectively tumour disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility.
Solvent-free direct enantioselective aldol reaction using polystyrene-supported N-sulfonyl-(Ra)-binam-d-prolinamide as a catalyst
Banon-Caballero, Abraham,Guillena, Gabriela,Najera, Carmen
experimental part, p. 1599 - 1606 (2010/12/25)
The immobilization of N-sulfonyl-(Ra)-binam-d-prolinamide using polystyrene as a support allows the recovery of an efficient catalytic system for the enantioselective direct aldol reaction between different ketones and aldehydes under solvent-f
Synthesis and structure-activity relationship studies on tryprostatin A, an inhibitor of breast cancer resistance protein
Jain, Hiteshkumar D.,Zhang, Chunchun,Zhou, Shuo,Zhou, Hao,Ma, Jun,Liu, Xiaoxiang,Liao, Xuebin,Deveau, Amy M.,Dieckhaus, Christine M.,Johnson, Michael A.,Smith, Kirsten S.,Macdonald, Timothy L.,Kakeya, Hideaki,Osada, Hiroyuki,Cook, James M.
, p. 4626 - 4651 (2008/09/21)
Tryprostatin A is an inhibitor of breast cancer resistance protein, consequently a series of structure-activity studies on the cell cycle inhibitory effects of tryprostatin A analogues as potential antitumor antimitotic agents have been carried out. These
Synthesis of microcolin analogs using trimethylsilylated lactams
Mattern, Ralph-Heiko,Gunasekera, Sarath P.,McConnell, Oliver J.
, p. 2197 - 2200 (2007/10/03)
The synthesis of microcolin analogs is described using an approach that could be of considerable practical interest for structure-activity studies on microcolin and related peptides. This synthetic pathway is more efficient than the methods reported to date, and allows the variation of the Xaa-pyrrolin-2-one unit of these molecules, which has been shown to be crucial for the biological activity.
