Mini Reviews in Medicinal Chemistry - Volume 11, Issue 8, 2011

The present review covers a concise account of the synthesis of bioactive 2, 3-disubstituted-quinazoline-4(3H)- ones and the recent developments in the area of versatile quinazolinones with a special emphasis on new synthetic routes and strategies.

Dihydro-oxadiazine and its derivatives have been demonstrated to be important heterocyclic scaffold platform with bioactive diversity, which present wide activities such as cardiovascular, antitumor, antibacterial, antimicrobial, acricidal, insecticidal, plant-growth regulating, chitin biosynthesis inhibitors and monoamine oxidase inhibition. Versatile features of dihydro-oxadiazine heterocycles have emerged, so the aim of the present paper was to review the recent advances of dihydro-oxadiazine-based heterocyclic derivatives mainly including synthesis and biological activities.

Small molecular weight substances are functional, as neurotrophic factors can be developed as therapeutic drugs to treat neurodegenerative disorder. Recently, a large number of natural and synthetic neuritogenic compounds have been discovered. These compounds have various structural features, including terpenoids, lipids, alkaloids, steroid glycosides, small molecular peptides, and so on. Some of them possess not only neurotrophic properties but also neuroprotective activities. The structure-activity relationships (SARs) and mechanism of action of some important compounds have been studied intensively. Increasing experimental evidence suggests that several of these compounds can be promising candidates for drug development.

The biological properties of the lanthanides, primarily based on their similarity to calcium, have been the basis for research into potential therapeutic applications of lanthanides since the early part of the twentieth century. Up to date, cerium nitrate has been used as a topical cream with silver sulfadiazene for the treatment of burn wounds. A lanthanide texaphyrin complex (motexafin gadolinium) has been evaluated through Phase III clinical trials for the treatment of brain metastases in non-small cell lung cancer. Lanthanum carbonate (Fosrenol) as a phosphate binder has been approved for the treatment of hyperphosphatemia in renal dialysis patients in both the USA and Europe. This review will highlight therapeutic applications of the lanthanides for burn wounds, cancer, hyperphosphatemia, immune function, magnetic resonance imaging (MRI) contrast agents and osteoporosis, and discuss their future potential in the medical fields.

The caffeic acid scaffold, which is abundant in nature, is extremely versatile and is found in a number of biologically active molecules. The purpose of this review is to provide an overview of the pharmacological activity of synthetic caffeic acid analogs including recent reports of anti-inflammatory, anti-cancer, and antiviral activities of these compounds.

Although 25 compounds are currently licensed as anti-HIV drugs, the development of multidrug-resistant viruses, as well as their severe side effects, compromise their efficacy and limit treatment options. The search for new targets in order to cure AIDS has revealed that the inhibition of some protein-protein interactions in the HIV life cycle may provide an important new approach to fight this disease. The interaction between HIV-1 integrase (IN) and Lens Epithelium-Derived Growth Factor (LEDGF/p75) has increasingly gained attention as a valuable target for a novel anti-retroviral strategy. This article reviews the discovery and development of molecules capable of interrupting the LEDGF/p75-IN interaction reported to date.