Medicinal Chemistry - Volume 7, Issue 2, 2011

Several protease inhibitors have reached the world market in the last fifteen years, dramatically improving the quality of life and life expectancy of millions of HIV-infected patients. In spite of the tremendous research efforts in this area, resistant HIV-1 variants are constantly decreasing the ability of the drugs to efficiently inhibit the enzyme. As a consequence, inhibitors with novel frameworks are necessary to circumvent res Read More

Local biosynthesis of estrogens, especially estradiol (E2), is thought to be important for the maintenance and growth of estrogen-sensitive diseases. To control E2 formation, we have investigated a series of epoxide and furanic E2 derivatives as inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1), the enzyme responsible for the conversion of estrone (E1) into E2. We report here a strategy to synthesize a series o Read More

5-aminosalicylic acid (5-ASA or mesalazine) is widely used for treatment of inflammatory bowel disease and considered to be cancer preventive. Still, the molecular mechanisms explaining its properties remain largely unknown, partially due to the lack of instrumentarium needed to identify its array of molecular targets. Modern OMICs-based technologies utilized in this study may serve as a powerful and unbiased tool to search Read More

Ethyl caffeate (EC), octyl caffeate(OC), benzyl caffeate(BC) and phenethyl caffeate(PC) were synthesized and evaluated for scavenging of superoxide anion, nitric oxide radical and 1,1-diphenyl-1-picrylhydrazyl radical(DPPH). Antioxidant activity was investigated with reducing power method. Pooled human liver microsome was used for investigating the effects on cytochrome P450 1A2 (CYP1A2) catalytic activities by Read More

Lung cancer is a leading cause of death in human. Cancer stem cells have been regarded as basis for failure of current therapeutic options. Salinomycin was shown to kill these cancer stem cells in some types of cancer such as breast cancer and leukemia. The in vitro anticancer activities of salinomycin have been validated against the lung cancer cell line A549 via sulforhodamine B and colony formation assay. Salinomycin Read More

The synthesis and antiproliferative activity of new coumarin-based benzopyranone derivatives containing basic amino side chain are described. The cytotoxicities against A549 and MCF-7 human cancerous cell lines were determined after 24, 48, 72h drug exposure employing MTT assay at concentrations ranging from 0-100 μM. The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4-hydro Read More

Human SP110 plays an important role in resisting intracellular pathogens, and hence has become an important drug target for preventing intracellular pathogen diseases, such as tuberculosis, hepatic veno-occlusive disease, and intracellular cancers. Unfortunately, so far little is known about the interactions of SP110 with the other proteins in a cell, which is considered to be the key for revealing its action mechanism an Read More

A series of 2-phenylbenzothiazoles has been synthesized either by i) condensation of different aromatic aldehydes with 2-aminothiophenol or ii) condensation of N-(2-chlorophenyl)benzothioamides in KOH catalyzed by potassium fericyanide. The structures of synthesized compounds were confirmed by IR, MS, and 1H-NMR. The results of biological activity screening showed that six compounds including 2-phenylbenzothiazol Read More

The reaction of a series of 1,2-diols with thionyl chloride led to bisnoradamantane sulfites in very good yields. The reaction has also been applied to related polycyclic scaffolds. The compounds have been tested for antiviral activity but none of them showed to be active. Several attempts to generate and trap SO from these polycyclic sulfites have been unsuccessful.

Dysfunction of the cochlea causes sensorineural hearing loss. Glucocorticoids have been clinically applied for sensorineural hearing loss of sudden onset, including idiopathic sudden sensorineural hearing loss, acoustic injury, Meniere's disease, and immune-mediated hearing loss. However, clinical studies on sudden sensorineural hearing loss have revealed conflicting results regarding the efficacy of glucocorticoids. The findi Read More