Current Topics in Medicinal Chemistry - Volume 13, Issue 17, 2013

A four-step approach for the synthesis of dihydroxylated piperidine, quinolizidine and indolizidine systems is described employing α,β-unsaturated diazoketones as versatile building blocks. Unsaturated diazoketones were readily prepared from a Horner-Wadsworth-Emmons reaction between a diazophosphonate and amino-aldehydes. The strategy employs an asymmetric dihydroxylation reaction as the key step and is simple an Read More

In order to overcome the significant side effects and the acquired resistance of platinum-based anticancer drugs, great efforts have been devoted to designing new platinum compounds or non-platinum transition metal anticancer complexes with improved pharmacological properties and a broader range of antitumor activity. Among them, the new complexes based on natural alkaloid and their derivatives provide a novel ap Read More

Aporphinoid alkaloids, which encompass a large number of complicated structures, are an important group of natural products. The anticancer activity of aporphinoid alkaloids has become a hot pharmaceutical research area in recent years. Recent studies on the anticancer activity of these compounds are reviewed. The structure activity relationships (SARs) and anticancer mechanisms of aporphinoid alkaloids, as well as sim Read More

In this study, antidepressant-like effects of intra-cerebroventricularly administration of oxoisoaporphine derivatives in post stroke-depressive like behavior were examined through despair swimming and tail suspension models. For this aim, acute ischemic stroke was induced by bilateral common carotid arteries occlusion which significantly changed the normal behaviors of male balb/c mice. We performed stroke-induced Read More

High molecular diversity of natural products (NPs) can provide a solution for many serious medicinal conditions. Frequently attributed with strong and useful biological/pharmacological properties, NPs may be directly applied in therapy, or could serve as templates for future drugs. As pain is a major symptom in many illnesses, and can significantly interfere with a person's quality of life and general functioning, pain-killing poten Read More

A great number of alkaloids exhibit high potential in cancer research. Some of them are anticancer drugs with well-defined clinical uses, exerting their action on microtubules dynamics or DNA replication and topology. On the other hand, mitochondria have been recognized as an essential organelle in the establishment of tumor characteristics, especially the resistance to cell death, high proliferative capacity and adaptation Read More

Alkaloids are interesting groups of natural products with important biological properties, but naturally available alkaloids are insufficient for biological studies. Therefore, the demand for higher amounts of alkaloids made research community to synthesize alkaloids by innovative techniques. The importance of asymmetric reactions for scientific community to obtain enantiomerically pure compounds with good yiel Read More

Argemone mexicana L. (Papaveraceae), accumulates benzylisoquinoline alkaloids, (BIA) derived from tyrosine. Although it was originated in the western region of the USA-Mexico border, it has spread to tropical and subtropical areas around the world. Today, it is used to treat different ailments, given to its antimicrobial, antiparasitic, antimalarial, pesticide, cytotoxic and neurological properties. These effects are related Read More

Cyclopamine is a naturally occurring steroidal alkaloid that attenuates the Hedgehog signaling pathway by inhibiting the Smoothened receptor. The Hedgehog pathway plays an important role in many human cancers. Cyclopamine has served as a pivotal tool compound in elucidating the pharmacological effect of the Hedgehog signaling pathway, however, due to its poor solubility, stability, and moderate activity, its clinica Read More