Results 21 to 30 of about 2,055 (188)

Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology [PDF]

, 2016
Targeting epigenetic proteins is a rapidly growing area for medicinal chemistry and drug discovery. Recent years have seen an explosion of interest in developing small molecules binding to bromodomains, the readers of acetyl-lysine modifications.
Alessio Ciulli, Carles Galdeano, Chiang C-M, Lejeune P   +3 more
core   +2 more sources

Enzyme-Catalysed Multicomponent Reactions (MCRs) for the Green Synthesis of Bioactive Heterocycles-A Review

Results in Chemistry
The increasing need for sustainable and eco-friendly chemical processes has driven considerable interest in biocatalysis and multicomponent reactions (MCRs) as greener approaches in organic synthesis.
Venkatesan K., Magdi E.A. Zaki, Sook-Keng Chang, Ling Shing Wong, Sobhi M. Gomha   +4 more
doaj   +1 more source

Gramine derivatives targeting Ca2+ channels and Ser/Thr phosphatases: A new dual strategy for the treatment of neurodegenerative diseases [PDF]

, 2016
This document is the unedited author's version of a Submitted Work that was subsequently accepted for publication in Journal of Medicinal Chemistry , copyright © American Chemical Society after peer review.
Alzheimer A., Carmen Nanclares, Chan S. F., Cristóbal de los Ríos, Juan-Alberto Arranz-Tagarro, Laura González-Lafuente, Luis Gandía, Mark R. J., Monique Araujo de Brito, Raquel L. Arribas, Rocío Lajarín-Cuesta, Settimo A. D.   +11 more
core   +3 more sources

Diazo Transfer From Nitrous Oxide Employing Phosphorus Ylides

Angewandte Chemie International Edition, EarlyView.
A phosphorus ylide‐mediated strategy achieves the direct fixation of nitrous oxide (N2O) to access diazo compounds, which after intra‐ or intermolecular trapping, afford N2‐containing organic building blocks. This approach provides an alternative to hazardous diazo‐transfer reagents and establishes N2O fixation as a sustainable methodology.
Jhen‐Kuei Yu, Jan Niclas Ludwig, Patrick Wolf Antoni, David Tymann, Max Martin Hansmann   +4 more
wiley   +1 more source

The discovery of I-BRD9, a selective cell active chemical probe for bromodomain containing protein 9 inhibition [PDF]

, 2016
Acetylation of histone lysine residues is one of the most well-studied post-translational modifications of chromatin, selectively recognized by bromodomain “reader” modules.
Andrew J. Bannister, Anne-Marie Michon, Antje Dittmann, Arrowsmith C. H., Bagnyukova T. V., Bamborough P., Baud M. G. J., Borah J. C., Brand M., Bunnage M. E., Chun-wa Chung, Chung C. W., Chung C. W., Chung C. W., Chung C. W., David H. Drewry, Dawson M. A., Demont E. H., Fedorov O., Ferguson F. M., Filippakopoulos P., Filippakopoulos P., Filippalopoulos P., Fish P. V., Furdas S. D., Gardner K. E., Garnier J. M., Gentile G., Gerard Drewes, Gosmini R., Guetzoyan L., Harner M. J., Hay D. A., Hewings D. S., Hewings D. S., Hewings D. S., Hohmann A. F., Hongbin S., Isabelle Becher, Jennings L. E., Judit Molnar, Ka Hing Che, Kadoch C., Knapp S., Laurie Gordon, Mathews T. P., Matthew Lindon, McKeown M. R., McLure K. G., Melanie Leveridge, Middeljans E., Mirguet O., Mirguet O., Morinière J., Mujtaba S., Müller S., Natalie H. Theodoulou, Nicholas C. O. Tomkinson, Nicodeme E., Paola Grandi, Paul Bamborough, Philip G. Humphreys, Picaud S., Prinjha R. K., Rab K. Prinjha, Rino A. Bit, Rooney T. P. C., Samuel C. Robson, Sanchez R., Sattler S., Scotto L., Seal J., Sweis R. F., Tony Kouzarides, Vollmuth F., Yan Y., Young R. J., Zeng L., Zhang G., Zhang S.   +79 more
core   +2 more sources

1,2‐Diazetidines − Structure, Synthesis, and Functionalization

European Journal of Organic Chemistry, EarlyView.
1,2‐Diazetidines are saturated four‐membered heterocycles featuring two adjacent nitrogen atoms. Despite recent advances in their synthesis and promising potential in medicinal chemistry, the chemistry of these cyclic hydrazines remains underexplored.
Stefan Roesner
wiley   +1 more source

Potent Fluorescent Probe for Target‐Engagement Studies of Allosteric Pyruvate Kinase Modulators

Angewandte Chemie, Volume 137, Issue 42, October 13, 2025.
LumiPK, a novel environment‐sensitive fluorescent tracer, enables direct monitoring of allosteric ligand engagement with pyruvate kinase fused with nanoluciferase (Nluc), focusing on the liver isoform (PKL). In NanoBRET, and fluorescence indicator displacement assays, LumiPK shows high affinity and validates known allosteric modulators of PKL.
Oscar Nilsson, Anna P. Valaka, Liliana Håversen, Agnieszka Bogucka, István Köteles, Paul Brear, Mikael Rutberg, Anders Gunnarsson, Marko Hyvönen, Morten Grøtli   +9 more
wiley   +2 more sources

Synthesis of 1-amino-4-(2´-thienyl)phthalazine derivatives [PDF]

, 2004
A synthesis of 1-amino substituted 4-(2´-thienyl)-phthalazines is described from halo- derivatives of 4-(2´-thienyl)-1-(2H)-phthalazinone 3.Fundação para a Ciência e Tecnologia. FEDER - POCTI (ref. POCTI/QUI/37816/2001)
Kirsch, G., Raposo, M. Manuela M., Sampaio, Ana M. B. A.   +2 more
core  

cardanol based green nanovesicles with antioxidant and cytotoxic activities [PDF]

, 2016
This manuscript describes the preparation of green nanovesicles by using cardanol as renewable starting material with embedded minor amounts of phthalazines, a class of heterocyclic bioactive compounds.
Diego Lomonaco, Ermelinda Bloise, Giuseppe Mele, Lucia Mergola, Luigi Carbone, Mohamed Sayed Behalo, Roberta Del Sole, Selma Elaine Mazzetto   +7 more
core   +1 more source

Dimethyl‐, Diethyl‐, and Propylene Carbonates: An Emerging Class of Green Solvents for Organic Synthesis

The Chemical Record, EarlyView.
This review highlights recent advances in the use of organic carbonates, dimethyl carbonate (DMC), diethyl carbonate (DEC), and propylene carbonate (PC), as solvents in organic synthesis. Based on over seventy studies from the past 6 years, it shows their application in different organic reaction types, emphasizing their role in safer and more ...
Gabriela T. Quadros, Livia C. L. Valente, Thiago Barcellos, Daniela Hartwig, Laura Abenante, Eder J. Lenardão   +5 more
wiley   +1 more source