- Stereoselective total synthesis of (-)-curvularin
-
A concise total synthesis of (-)-Curvularin have been synthesized from commercially available (S)-(?)-propylene epoxide and (3,5-Dimethoxyphenyl)acetic acid. The key steps involved in the synthesis are Vilsmeier-Haack formylation, Grignard reaction, alkyl
- Jayaprakash, H. V.,Radha Krishna, Muniganti,Sridhar, Gattu,Syed, Tasqeeruddin
-
supporting information
(2021/12/22)
-
- Xylochemical synthesis and biological evaluation of shancigusin c and bletistrin g
-
The biological activities of shancigusin C (1) and bletistrin G (2), natural products isolated from orchids, are reported along with their first total syntheses. The total synthesis of shancigusin C (1) was conducted by employing the Perkin reaction to forge the central stilbene core, whereas the synthesis of bletistrin G (2) was achieved by the Wittig olefination followed by several regiose-lective aromatic substitution reactions. Both syntheses were completed by applying only renewable starting materials according to the principles of xylochemistry. The cytotoxic properties of shancigusin C (1) and bletistrin G (2) against tumor cells suggest suitability as a starting point for further structural variation.
- Efferth, Thomas,Geske, Leander,Kauhl, Ulrich,Opatz, Till,Saeed, Mohamed E. M.,Schüffler, Anja,Thines, Eckhard
-
supporting information
(2021/06/16)
-
- Synthesis of (+)-xestodecalactone A
-
The total synthesis of Benzannulated macrolide, (+)-Xestodecalactone A was accomplished starting from commercially available enantiomerically pure propylene oxide and 3,5-dihydroxyphenylacetic acid using Grignard reaction, alkylation of 1,3-dithiane and Y
- Mura Reddy, Gudisela,Prasad, K. R. S.,Reddy, G. Nagendra,Sridhar, Gattu
-
supporting information
(2021/06/27)
-
- Identification of N,N-arylalkyl-picolinamide derivatives targeting the RNA-binding protein HuR, by combining biophysical fragment-screening and molecular hybridization
-
Hu proteins are members of the RNA-binding protein (RBP) family and play a pivotal role in the regulation of post-transcriptional processes. Through interaction with selected mRNAs, RBPs regulate their function and stability; as a consequence, RBP dysregu
- Della Volpe,Linciano,Listro,Tumminelli,Amadio,Bonomo,Elgaher,Adam,Hirsch,Boeckler,Vasile,Rossi,Collina
-
-
- Concise Total Synthesis of Curvulone B
-
A concise and convergent stereoselective synthesis of curvulone B is described. The synthesis utilized a tandem isomerization followed by C-O and C-C bond-forming reactions following Mukaiyama-Type aldol conditions for the construction of the trans-2,6-di
- Banoth, Shivalal,Choudhury, Utkal Mani,Marumudi, Kanakaraju,Kunwar, Ajit C.,Mohapatra, Debendra K.
-
supporting information
p. 685 - 688
(2020/12/07)
-
- Blue Light-Promoted N?H Insertion of Carbazoles, Pyrazoles and 1,2,3-Triazoles into Aryldiazoacetates
-
Blue light irradiation of aryldiazoacetates leads to the formation of free carbenes, which can react with carbazoles, pyrazoles and 1,2,3-triazoles to afford the corresponding N?H inserted products. These reactions are performed under air and at room temperature, allowing the mild preparation of a variety of motifs found in biologically relevant targets. (Figure presented.).
- Stivanin, Mateus L.,Fernandes, Alessandra A. G.,da Silva, Amanda F.,Okada, Celso Y.,Jurberg, Igor D.
-
supporting information
p. 1106 - 1111
(2020/01/25)
-
- Room Temperature Coupling of Aryldiazoacetates with Boronic Acids Enhanced by Blue Light Irradiation
-
A visible-light-promoted photochemical protocol is reported for the coupling of aryldiazoacetates with boronic acids. This photochemical reaction shows great enhancement compared to the same protocol performed in the absence of light. Except for a few cases, the room temperature coupling in the dark (thermal process) generally does not work. When it does, it is likely to also involve free carbenes as key intermediates. Alternatively, photochemical reactions show a broad scope, can be performed under air and tolerate a wide variety of functional groups. Reaction-evolution monitoring, DFT calculations and control experiments have been used to evaluate the main aspects of this intricate mechanistic scenario. Biologically active molecules Adiphenine, Benactyzine and Aprophen have been prepared as examples of synthetic applications.
- da Silva, Amanda F.,Afonso, Marco A. S.,Cormanich, Rodrigo A.,Jurberg, Igor D.
-
supporting information
p. 5648 - 5653
(2020/04/22)
-
- A Unified Synthetic Approach to Optically Pure Curvularin-Type Metabolites
-
A unified and concise approach to the synthesis of nine curvularin-type metabolites and two analogues has been developed with few steps and high yields. Among them, sumalactones A-D were synthesized for the first time. The key steps in this approach inclu
- Allu, Srinivasa Rao,Banne, Sreenivas,Jiang, Jia,Qi, Na,Guo, Jian,He, Yun
-
p. 7227 - 7237
(2019/06/07)
-
- PROCESSES FOR PREPARING AN FGFR INHIBITOR
-
Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-l-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2- (methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.
- -
-
Page/Page column 27-28
(2017/03/17)
-
- Inhibitors of the fibroblast growth factor receptor
-
Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of FGFR-4.
- -
-
Page/Page column 49
(2017/08/01)
-
- QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS
-
Compounds of formula (I) that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
- -
-
Page/Page column 59
(2016/12/16)
-
- Syntheses of cytosporones A, C, J, K, and N, metabolites from medicinal fungi
-
The syntheses of the fungal metabolites cytosporones A, (±)-C, and N are reported. And the syntheses of cytosporones J and K are described for the first time. The preparation of racemic cytosporone J and racemic cytosporone K, natural products containing
- Beekman, Andrew M.,Barrow, Russell A.
-
p. 1583 - 1592
(2015/10/20)
-
- QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS
-
Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for
- -
-
Page/Page column 129
(2015/09/23)
-
- CHEMICAL COMPOUNDS ACTING AS PERK INHIBITORS
-
The invention is directed to substituted pyrrolidinone derivatives. Specifically, the invention is directed to compounds according to Formula X: wherein R41, R42, R43, R44, R45, R46, and R47 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, diabetes, Parkinson disease, Huntington's disease, Creutzfeldt- Jakob Disease, and related prion diseases, amyotrophic lateral sclerosis, myocardial infarction, neurodegeneration, cardiovascular disease, atherosclerosis, ocular diseases, and arrhythmias, more specifically cancers of the breast, colon, pancreas and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
- -
-
Page/Page column 115
(2015/10/05)
-
- INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
-
Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of FGFR-4.
- -
-
Paragraph 0172; 0173
(2015/07/22)
-
- QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR INHIBITORS
-
Compounds of formula (Ι') that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
- -
-
Page/Page column 57
(2014/12/09)
-
- INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
-
Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
- -
-
Page/Page column 31; 32; 33
(2014/02/15)
-
- First syntheses of the biologically active fungal metabolites pestalotiopsones A, B, C and F
-
A synthetic approach accessing the pestalotiopsones, fungal chromones possessing a rare skeletal subtype, is reported for the first time. The synthesis of pestalotiopsone A (1) has been achieved in 7 linear steps (28%), from commercially available 3,5-dim
- Beekman, Andrew Michael,Castillo Martinez, Edwin,Barrow, Russell Allan
-
p. 1109 - 1115
(2013/03/28)
-
- Stereochemical assignment of the fungal metabolites pestalotiopsones D and e through enantiopure synthesis
-
The pestalotiopsones are fungal metabolites isolated from an endophytic fungus Pestalotiopsis sp. found in the mangrove Rhizophora mucronata, used in traditional Chinese medicine to treat symptoms of dysentery. The absolute configurations of pestalotiopso
- Beekman, Andrew Michael,Barrow, Russell Allan
-
p. 2054 - 2059
(2014/01/06)
-
- TREATMENT OF DISEASES BY EPIGENETIC REGULATION
-
The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.
- -
-
Paragraph 0471
(2013/11/05)
-
- COMPOUNDS FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASES
-
The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
- -
-
Page/Page column 32-33
(2008/12/07)
-
- Rational design of inhibitors of VirA-VirG two-component signal transduction
-
VirA-VirG two-component system regulates the vir (virulence) operon in response to specific host factors (xenognosins) in the plant pathogen Agrobacterium tumefaciens. Using whole cell assays, stable inhibitors inspired by the labile natural benzoxazinone inhibitor HDMBOA are developed. It is found that aromatic aldehydes represent a minimal structural unit for activity. In particular, 3-hydroxy-4,6-dimethoxy-3H-isobenzofuran-1-one (HDI) was found to have the highest activity, making it the most potent developed inhibitor of virulence gene expression in Agrobacterium.
- Maresh, Justin,Zhang, Jin,Tzeng, Yih-Ling,Goodman, Nora A.,Lynn, David G.
-
p. 3281 - 3286
(2008/02/08)
-
- PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF COMPLEX DISEASES AND THEIR DELIVERY BY INSERTABLE MEDICAL DEVICES
-
The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.
- -
-
Page/Page column 105-106
(2008/06/13)
-
- The first asymmetric total syntheses and determination of absolute configurations of xestodecalactones B and C
-
The first efficient asymmetric total syntheses of xestodecalactones B and C have been accomplished in 10 steps with an overall yield of 22 and 20.2%, respectively. The key steps involve the utility of Evans oxazolidinone-mediated syn-aldol condensations to establish the C-9 configuration and the macrolide ring formation by intramolecular acylation. The absolute configurations of xestodecalactones B and C have been determined via these syntheses.
- Liang, Qiren,Zhang, Jiyong,Quan, Weiguo,Sun, Yongquan,She, Xuegong,Pan, Xinfu
-
p. 2694 - 2697
(2007/10/03)
-
- Novel dihydropyridinone compounds
-
Disclosed are novel dihydropridinone compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon lung and prostate tumors. Also, disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.
- -
-
Page/Page column 13
(2010/02/07)
-
- An efficient synthesis of 3,5-dimethoxyhomophthalic acid, a key intermediate for synthesis of natural isocoumarins
-
3,5-Dimethoxyhomophthalic acid was prepared efficiently in three steps, from 3,5-dimethoxybenzyl bromide via rhodium-catalyzed direct carbonylation to 3,5-dimethoxyphenylacetic acid followed by successive o-formylation and oxidation. Isocoumarins related
- Saeed, Aamer,Rama, Nasim H.,Arfan
-
p. 519 - 522
(2007/10/03)
-
- 1,2-disubstituted-6-oxo-3-phenyl-piperidine-3-carboxamides and combinatorial libraries thereof
-
The invention relates to combinatorial libraries containing two or more novel piperidine-3-carboxamide derivative compounds, methods of preparing the piperidine-3-carboxamide derivative compounds and piperidine-3-carboxamide derivative compounds bound to a resin
- -
-
-
- Synthesis of 3,5-dihydroxyphenylglycine derivatives and the C-terminal dipeptide of vancomycin
-
Syntheses of optically active 3,5-DMPG and racemic 3,5-DHPG, the latter suitably protected for incorporation into linear peptides modelled on vancomycin, are described and a synthesis of the optically pure protected C-terminal dipeptide of vancomycin is p
- Stone, Martin J.,Maplestone, Rachael A.,Man, Shirley K. Rah,Williams, Dudney H.
-
p. 2663 - 2666
(2007/10/02)
-
- Melanin Biosynthesis: A Study of Polyphenol Deoxygenation
-
The 1,3,6,8-Tetrahydroxynaphthalene (T4HN) reductase of Verticillium dahliae has been studied in a cell-free system.The use of specifically labelled 4(R)- and NADPH in the reduction of T4HN to scytalone reveals that the l
- Viviani, Fabrice,Gaudry, Michel,Marquet, Andree
-
p. 1255 - 1259
(2007/10/02)
-
