Mini Reviews in Medicinal Chemistry - Volume 10, Issue 13, 2010

The chemistry of pyrazoloquinolines is well established. This system has proved to be a very attractive scaffold for medicinal chemist in the recent past. Pyrazoloquinolines were extensively studied as bioactive compounds and are known to possess remarkable biological activities such as anti-cancer, anti-anxiety, anti-inflammatory, anti-asthmatic, cerebroprotective and anti-viral among others. For many of the activities the mo Read More

Inhibitors of thymidylate synthase (TS) play an essential role in the pharmacological management of several tumors. Two antifolates, Raltitrexed and Pemetrexed, are licensed anticancer drugs, with Pemetrexed, unlike Raltitrexed, undergoing further intense clinical development. Other antifolate TS inhibitors, recently/currently tested in clinical studies, that show encouraging anticancer activities are Plevitrexed, GW7904 Read More

Chromatography technology has been widely applied in various aspects of the pharmacy research on traditional Chinese medicine (TCM). This paper reviews literatures, published in the past decades, on the separation of active component from TCM using chromatography technology. Ultra-performance liquid chromatography (UPLC), high-speed counter-current chromatography (HSCCC), rapid resolution liquid chromatograp Read More

Alkaloids are a group of natural products with unmatched chemical diversity and biological relevance forming potential quality pools in drug screening. The molecular aspects of their interaction with many cellular macromolecules like DNA, RNA and proteins are being currently investigated in order to evolve the structure activity relationship. Isoquinolines constitute an important group of alkaloids. They have ext Read More

This review discusses the most active natural and synthetic curarelike compounds demonstrating myorelaxants activity. The data are grouped according to chemical structures, namely, quinoline and isoquinoline myorelaxants, myorelaxants with saturated heterocyclic or alkylamine fragments, myorelaxants with a steroid framework, natural and synthetic alkaloid myorelaxants.

Histone Deacetylases (HDACs) enzymes are critical in regulating gene expression and transcription. They also play a fundamental role in regulating cellular activities such as cell proliferation, survival and differentiation. Inhibition of HDACs has generated many fascinating results including a new strategy in human cancer therapy. HDAC Inhibitors (HDACIs) like SAHA, TSA are emerging as new promising drugs for various anti-infla Read More

CCR5 (C-C chemokine receptor type 5) is a chemokine receptor that has been identified as a major HIV coreceptor in viral entry and therefore is a highly validated target for the development of new anti-HIV drugs. Here, we discuss the insights gained so far relevant to the development of small-molecule CCR5 inhibitors for the treatment of HIV, and highlight small-molecule CCR5 inhibitors that are currently under preclinical and Read More