In this critical review the applications of gold catalysed reactions in total synthesis during the years since our last article are reviewed. At the end of this article a literature analysis is conducted to evaluate the progress in this field.

Gold catalysis in total synthesis – recent achievements

A review on recent developments of indole-containing antiviral agents.

In recent years, organocatalysis has enhanced its importance as a tool for the synthesis of enantiomerically enriched compounds. Among the candidates for organocatalysis, the construction of asymmetric quaternary carbons is regarded as a challenging problem in organic synthesis. In particular, 3,3′-disubstituted oxindoles have one or more asymmetric quaternary carbon atoms and they represent a large family of bioactive compounds and synthetic derivatives that mimicry natural products. Therefore they are good targets for drug candidates and in the last two years many papers have appeared on organocatalytic methods for the synthesis of 3,3′-disubstituted oxindoles. Moreover, in the last few years 2-substituted and 2,2′-disubtituted 3-indolinones have also attracted the interest of chemists. This review aims to cover the literature on these topics from its origin to the end of 2011.

Recent advances in organocatalytic methods for the synthesis of disubstituted 2- and 3-indolinones

3.1. Biosynthesis from Jatrophanes 4313 3.2. Biosynthesis from Lathyranes 4314 4. Biological Activity 4314 4.1. Antiproliferative Activity 4314 4.2. Cytotoxicity 4316 4.3. Effects on the Cell Division 4316 4.4. DNA-Damaging Activity 4316 4.5. Modulatority of Multidrug Resistance 4316 4.6. Tumor Promoting Activity 4318 4.7. Pro-Inflammatory Activity 4318 4.8. Inhibition of Allergic Reactions 4318 4.9. Antimicrobial Activity 4319 4.10. Antidiarrheal Activity 4322 4.11. Antipyretic-Analgesic Activity 4322 4.12. Molluscicidal and Antifeedant Activities 4323 4.13. Inhibitory Activity on the Mammalian Mitochondrial Respiratory Chain 4323

Chemical and Pharmacological Research of the Plants in Genus Euphorbia

Indoles as therapeutics of interest in medicinal chemistry: Bird's eye view.

Three new indole alkaloids from Trigonostemon lii.

A series of novel thioether pleuromutilin derivatives incorporating various heteroaromatic substituents into the C14 side chain have been reported. Structure-activity relationship (SAR) studies resulted in compounds 52 and 55 with the most potent in vitro antibacterial activity among the series (MIC = 0.031-0.063 μg/mL). Further optimization to overcome the poor water solubility of compound 55 resulted in compounds 87, 91, 109, and 110 possessing good in vitro antibacterial activity with increased hydrophilicity. Compound 114, the water-soluble phosphate prodrug of compound 52, was also prepared and evaluated. Among the derivatives, compound 110 showed moderate pharmacokinetic profiles and good in vivo efficacy in both MSSA and MRSA systemic infection models. Compound 110 was further evaluated in CYP450 inhibition assay and displayed intermediate in vitro inhibition of CYP3A4.

Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.

L-proline-catalyzed asymmetric aldol condensation of several isatin derivatives with acetone is reported. The desired products were obtained in highly yield with the ee among 30-79%. The substitutes of N can deeply effect the ee value of products, and a novel mechanism is also described.

Suo Gao

Papers

Three new indole alkaloids from Trigonostemon lii.

Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.

L-proline-catalyzed asymmetric aldol condensation of N-substituted isatins with acetone

Cipadonoid A, a novel limonoid with an unprecedented skeleton, from Cipadessa cinerasecns.

New phenanthrenes from Trigonostemon lii Y.T. Chang