RESUMO
The first asymmetric total synthesis of the tricyclic diterpenoid natural product (-)-dolastatrienol has been accomplished using a rhodium(II)-catalyzed carbene cyclization cycloaddition cascade reaction as the key step to construct the [5.4.0]carbobicyclic core. An intramolecular Heck reaction furnished the tricyclic skeleton and a challenging methylenation completed the synthesis of the target.
RESUMO
Correction for 'Virtual screening and optimization of Type II inhibitors of JAK2 from a natural product library' by Dik-Lung Ma et al., Chem. Commun., 2014, 50, 13885-13888.
RESUMO
Amentoflavone has been identified as a JAK2 inhibitor by structure-based virtual screening of a natural product library. In silico optimization using the DOLPHIN model yielded analogues with enhanced potency against JAK2 activity and HCV activity in cellulo. Molecular modeling and kinetic experiments suggested that the analogues may function as Type II inhibitors of JAK2.
Assuntos
Antivirais/farmacologia , Produtos Biológicos/farmacologia , Avaliação Pré-Clínica de Medicamentos , Janus Quinase 2/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Bibliotecas de Moléculas Pequenas/farmacologia , Antivirais/química , Produtos Biológicos/química , Hepacivirus/efeitos dos fármacos , Humanos , Janus Quinase 2/metabolismo , Cinética , Modelos Moleculares , Estrutura Molecular , Inibidores de Proteínas Quinases/química , Bibliotecas de Moléculas Pequenas/químicaRESUMO
The pseudolaric acids are diterpenoids isolated from the root bark of Pseudolarix amabilis, or the golden larch. Pseudolaric acids A and B are the major antifungal and anti-angiogenic congeners of this family of compounds. This review presents the results of the isolation, biological and synthetic studies of these natural products. 127 references are cited.
Assuntos
Produtos Biológicos , Diterpenos , Medicamentos de Ervas Chinesas , Inibidores da Angiogênese , Anti-Infecciosos , Antineoplásicos Fitogênicos , Produtos Biológicos/síntese química , Produtos Biológicos/química , Produtos Biológicos/isolamento & purificação , Produtos Biológicos/farmacologia , Anticoncepcionais , Diterpenos/síntese química , Diterpenos/química , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Medicamentos de Ervas Chinesas/síntese química , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Estrutura Molecular , Relação Estrutura-AtividadeRESUMO
[reactions: see text] [(Ph3P)CuH]6 effectively catalyzes the hydrostannation of activated alkynes with exclusive regioselectivity for alpha-stannation. Syn hydrostannation is observed exclusively for alkynoates. Anti or syn hydrostannation adducts are obtained as products for alkynone substrates.
