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BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
TLDR
Proteolysis targeting chimera (PROTAC) degraders of the BAF ATPase subunits SMARCA2 andSMARCA4 are developed using a bromodomain ligand and recruitment of the E3 ubiquitin ligase VHL to degrade high profile drug targets and induce cancer cell death. Expand
Circulating procoagulant microparticles in cancer patients
TLDR
Levels of microparticles were elevated in cancer patients compared to healthy individuals in this study, however, elevated MP levels were not predictive of VTE. Expand
Application of the Rodriguez-Pattenden photo-ring contraction: total synthesis and configurational reassignment of 11-gorgiacerol and 11-epigorgiacerol.
A stereospecific photochemical ring contraction was used as the key step in the first total synthesis of the marine pseudopteranyl diterpene 11-gorgiacerol and its 11-epimer. The synthesis allowedExpand
Synthesis of the lycopodium alkaloid (+)-lycoflexine.
TLDR
This synthesis covers four one-pot reactions, including a tandem Sakurai/aldol sequence, a novel hydroboration/oxidation procedure, a deprotection/transannular Mannich reaction, and a tandem catalysis cascade combining an enynene ring-closing metathesis and a selective hydrogenation. Expand
Total Synthesis of (+)-Linoxepin by Utilizing the Catellani Reaction**
TLDR
Lignans exhibiting immunosuppressive activity, tumor growth inhibition, and anti-fungal properties have been used in disease therapy, such as the anticancer agent etoposide. Expand
Additive effects in the palladium-catalyzed carboiodination of chiral N-allyl carboxamides.
TLDR
The finding that tertiary amines act as weakly coordinating ligands which significantly enhance diastereoselectivity in the Pd/QPhos-catalyzed carboiodination of chiral N-allyl carboxamides is presented. Expand
Intermolecular domino reaction of two aryl iodides involving two C-H functionalizations.
A palladium-catalyzed intermolecular cross-coupling of two aryl iodides is reported, giving polycyclic ring systems with a high level of convergence and efficiency.
Discovery of Novel Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2-p53 Interaction.
TLDR
Novel, chemically stable spiro-oxindole compounds bearing a spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-one scaffold that show in vivo efficacy in a SJSA-1 xenograft model even when given as a single dose. Expand
Application of the Palladium‐Catalysed Norbornene‐Assisted Catellani Reaction Towards the Total Synthesis of (+)‐Linoxepin and Isolinoxepin
Our ongoing effort towards the development of highly selective transition-metal-catalysed C-H activation processes has led to the expansion of the Catellani reaction. In a Pd-0/Pd-II/Pd-IV-catalysedExpand
Telechelic Poly(N-isopropylacrylamides) via Nitroxide-Mediated Controlled Polymerization and “Click” Chemistry: Livingness and “Grafting-from” Methodology
We report on the synthesis of telechelic poly(N-isopropylacrylamides) (PNIPAM) via nitroxide-mediated controlled polymerization, putting a focus on the introduction of defined end group moieties in...
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