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Enantiopure Indolizinoindolones with in vitro Activity against Blood‐ and Liver‐Stage Malaria Parasites
TLDR
An (S)‐tryptophanol‐derived isoindolinone was identified as a promising starting scaffold to search for novel antimalarials, combining excellent activity against both stages of the parasite′s life cycle with low cytotoxicity and excellent metabolic and chemical stability in vitro.
Synthetic Condensed 1,4-naphthoquinone Derivative Shifts Neural Stem Cell Differentiation by Regulating Redox State
TLDR
Exposure to 1a shifts NSC differentiation potential from neurogenic to gliogenic lineage and involves the generation of reactive oxygen species, without increasing cell death, and support a new role for a specific naphthoquinone derivative in NSC fate decision.
Michael acceptors as cysteine protease inhibitors.
TLDR
This review emphasizes on the new developments from literature reports on Michael acceptors as potential cysteine protease inhibitors, namely vinyl sulfones, alpha,beta-unsaturated carbonyl derivatives and aza-peptides.
Enhancing macrocyclic diterpenes as multidrug-resistance reversers: structure-activity studies on jolkinol D derivatives.
TLDR
In this small library of novel bioactive macrocyclic lathyrane diterpene derivatives, designed to evaluate structure-activity relationships essential in overcoming multidrug resistance (MDR), some correlations between MDR reversal and molecular weight, accessible solvent areas, and octanol/water partition coefficient were identified that can contribute to the development of new selective P-gp reversal agents.
Straightforward methodology for the enantioselective synthesis of benzo[a]- and indolo[2,3-a]quinolizidines.
TLDR
An enantioselective two-step route to substituted benzo[a]- and indolo[2,3-a]quinolizidines has been developed and takes advantage of the masked N-acyl iminium ion present in the resulting oxazolopiperidone lactams.
Enantioselective spirocyclizations from tryptophanol-derived oxazolopiperidone lactams.
A straightforward synthetic route to enantiopure spiro[indole-3,3'-indolizidines] is reported. The key step is a Lewis acid promoted cyclization of a Na-tosyltryptophanol-derived oxazolopiperidone
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