Current Medicinal Chemistry - Volume 16, Issue 17, 2009

Although chemotherapy is considered the mainstay of cancer therapy, unfortunate side effects of chemotherapy create a continuous demand for developing other novel and specific targets for cancer therapy. Re-expression of epigenetically silenced tumor suppressor genes is a rational strategy for the treatment of human neoplasms. Epigenetic modifiers like DNA methyltransferase (DNMT) inhibitors and histone deactey Read More

Benzamide derivatives are known as antipsychotic and antiemetic drugs. Owing to its neurotropic characteristic this class of compounds was found useful for imaging melanoma and melanoma metastases. [123I]BZA (N-(2- diethylaminoethyl)-4-[123I]iodobenzamide) was the first example which was clinically applied as an imaging agent demonstrating high tumor uptake. This finding initiated research efforts to further improve th Read More

Protein tyrosine phosphatases (PTPs) play a critical role in physiological signaling pathways by controlling the level of tyrosine phosphorylation. The past decade has seen a vast increase in both academic and industrial interest in PTPs and their relevance as potential therapeutic targets, with several PTP inhibitors recently entering clinical trials. Despite these developments, there are numerous examples of failed PTP drug disc Read More

During more than five decades, pyridinium oximes have been developed as therapeutic agents used in the medical treatment of poisoning with organophosphorus compounds. Their mechanism of action is reactivation of acetylcholinesterase (AChE) inhibited by organophosphorus agents. Organophosphorus compounds (OPC) are used as pesticides and developed as warfare nerve agents such as tabun, soman, sarin, VX a Read More

The anticonvulsant and neuroprotective properties of agonist and antagonist of metabotropic glutamate receptors (mGluRs ) have been known for 15 years or so. However, it is not yet clear whether these agents, and allied compounds, can be considered as candidate drugs for eventual use in the clinic to control the development of epilepsy, (i.e. as anti- epileptogenics), or for the control of seizures themselves (i.e. as anticonvu Read More

Carbazole derivatives are well known for their various pharmacological activities, including anti-HIV, anticancer, antibacterial and antifungal activities. This review will focus on carbazoles that possess antifungal activity against Candida albicans, the major human fungal pathogen. In our search for new fungicidal compounds, we identified a series of substituted carbazoles, termed N-alkylated 3,6-dihalogenocarbazoles, tha Read More