A Biocatalytic Platform for Synthesis of Chiral α-Trifluoromethylated Organoborons [PDF]
, 2018 There are few biocatalytic transformations that produce fluorine-containing molecules prevalent in modern pharmaceuticals. To expand the scope of biocatalysis for organofluorine synthesis, we have developed an enzymatic platform for highly ...
Arnold, Frances H. +6 more
core +3 more sources
2,20-Dihydroxybenzophenones and their carbonyl N-analogues as inhibitor scaffolds for MDR-involved human glutathione transferase isoenzyme A1-1 [PDF]
, 2014 The MDR-involved human GSTA1-1, an important isoenzyme overexpressed in several tumors leading to chemotherapeutic-resistant tumour cells, has been targeted by 2,2′-dihydroxybenzophenones and some of their carbonyl N-analogues, as its potential ...
Clonis, Yannis D. +7 more
core +1 more source
A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors [PDF]
, 2018 Crystallography has guided the hybridization of two series of Trypanosoma brucei N-myristoyltransferase (NMT) inhibitors, leading to a novel highly selective series.
Brand, Stephen +18 more
core +3 more sources
Antiprotozoal glutathione derivatives with flagellar membrane binding activity against T. brucei rhodesiense. [PDF]
, 2016 A new series of N-substituted S-(2,4-dinitrophenyl)glutathione dibutyl diesters were synthesized to improve in vitro anti-protozoal activity against the pathogenic parasites Trypanosoma brucei rhodesiense, Trypanosoma cruzi and Leishmania donovani.
Croft, Simon L +3 more
core +2 more sources
Chemoenzymatic approach toward the synthesis of 3-O-(α/β)-glucosylated 3-hydroxy-β-lactams [PDF]
, 2018 Glycosylation significantly alters the biological and physicochemical properties of small molecules. beta-Lactam alcohols comprise eligible substrates for such a transformation based on their distinct relevance in the chemical and medicinal community. In
D'hooghe, Matthias +8 more
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Recent Advances in Biocatalytic Promiscuity: Hydrolase-Catalyzed Reactions for Nonconventional Transformations [PDF]
, 2015 Financial support from the Spanish Ministerio de Economía y Competitividad (CTQ2013-44153-P) is grateful acknowledged. M.L.-I.
Gotor Fernández, Vicente +1 more
core +2 more sources
The selective cytotoxicity of the alkenyl glucosinolate hydrolysis products and their presence in Brassica vegetables. [PDF]
, 2015 © 2015 Elsevier Ireland Ltd.Cruciferous vegetable consumption correlates with reduced risk of cancer. This chemopreventative activity may involve glucosinolates and their hydrolysis products.
David, R +3 more
core +1 more source
Phosphoramidates and phosphonamidates (ProTides) with antiviral activity [PDF]
, 2018 Following the first report on the nucleoside phosphoramidate (ProTide) prodrug approach in 1990 by Chris McGuigan, the extensive investigation of ProTide technology has begun in many laboratories.
Arbelo RC +9 more
core +2 more sources
Review of QSAR Models and Software Tools for predicting Acute and Chronic Systemic Toxicity [PDF]
, 2010 Information on acute and chronic systemic toxicity, arising from the oral, dermal and inhalation routes of exposure, are key elements in the regulatory assessment of chemicals. Traditionally, this information is obtained from animal studies. However, due
FUART GATNIK Mojca +2 more
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Archiv der Pharmazie, Volume 359, Issue 2, February 2026.We identified a novel N9‐substituted harmine analog, compound 6, that selectively suppresses leukemic cell growth, triggers DNA damage, and activates apoptosis while sparing healthy fibroblasts. This discovery highlights N9‐modified β‐carbolines as a powerful new class of selective antileukemic agents, bridging natural product chemistry with next ...
Abdul Aziz Timbilla +17 more
wiley +1 more source