Medicinal Chemistry - Volume 2, Issue 6, 2006

Uncontrolled kallikrein activation is involved in diseases such as hereditary angioedema, bacterial septic shock and procedures such as cardiopulmonary bypass. Here we report a series of small molecule compounds that potently inhibit kallikrein activity in vitro. Kinetic studies indicate that some of these compounds are slow binding inhibitors of kallikrein with Ki final less than a nanomolar. The ability of these co Read More

Despite the importance of embryonic stem cells in embryology and regenerative medicine, their response to DNA damage is not fully understood. Here we studied the expression profiles of small RNAs approximately 22 nucleotides long called micro RNAs, which play an important role in developmental regulation in plants and animals. We identified a group of micro RNAs with increased expression after exposure to radiati Read More

Physicochemical characteristics of two structurally different cage dimeric 1,4-dihydropyridines HX (1) and CC (2) have been determined and compared to their P-glycoprotein inhibiting properties. While the weakly basic compound (1) showed pH-dependent apparent partition coefficients (log D), the neutral compound (2) proved to have almost identical log D values at varying pH-values. The subsequent determination of p Read More

Recent studies have indicated that minor functional changes on the steroidal part of complex molecules, comprising of an alkylating moiety and a steroidal congener, lead to compounds with enhanced biological activity. The observed induction of the genotoxic, cytotoxic and antileukemic effects suggest a determinative role of the steroidal congener on the mechanism of action. In order to further elucidate the structural r Read More

A series N-[4-(1H(2H)-benzotriazol-1(2)-yl)phenyl]alkylcarboxamides (8e-k, 9e-i, k, l) and their parent amines (5a-c and 6a-d) were prepared according to Schemes (1 and 2). Compounds were evaluated in vitro for cytotoxicity and antiviral activity against a wide spectrum of RNA (positive- and negative-sense) viruses, like [Bovine Viral Diarrhea Virus (BVDV), Yellow Fever Virus (YFV), Coxsackie Virus B (CVB-2), Polio Virus (Sb- Read More

We have recently presented the synthesis of 2-amino-1,4-benzoquinones by nuclear amination of phydroquinones with primary aromatic amines using fungal laccases as catalysts. In the present report, a series of selected 2-amino-1,4-benzoquinones was tested for biological activities, such as inhibition of human 5-lipoxygenase and antiproliferative/ anti-neoplastic effects. Compound 9 (2-[4'-(iso-propylphenyl)-amino]-5,6-dimet Read More

We recently identified two compounds of 5-benzylidene-2-phenylimino-1,3-thiazolidin-4-one (BPT) analog, 5- (4-methylbenzylidene)-2-phenylamino-1,3-thiazolidin-4-one (MMPT) and 5-(2,4-dihydroxybenzylidene)-2-phenylimino- 1,3-thiazolidin-4-one (DBPT), that can effectively induce apoptosis in cancer cells but not in normal cells, independently of P-glycoprotein status. To further investigate the antitumor activity of BPT analogs, Read More

Purpose: To determine persitent organic pollutants in adipose tissue in a patient with kidney cancer. Methods: Adipose tissue was sampled from the abdominal wall during autopsy of a 75-year old man who had died from a kidney cancer. The concentrations of polychlorinated biphenyls (PCBs), p,p'-dichlorodiphenyltrichloroethane (DDE), hexachlorobenzene (HCB), chlordanes and tetrabromodiphenyl ether (TeBDE) were determin Read More

Objective: To study the effects of interleukin-10 on the expression of fas and fasL in hepatic stellate cells in experimental rat hepatic fibrosis. Methods: Sixty clean SD rats were divided into control group (8 in group N), the model group (28 in group C) and the IL- 10 treated group (24 in group I) randomly. The rats were administered CCl4 with or without IL-10 treatment. Hepatic stellate cells (HSCs) were isolated from the Read More

Two new series of N4-(2, 5-disubstitutedphenyl) semicarbazones were synthesized and evaluated for the anticonvulsant activity in various animal models of seizures. Quantum mechanical modeling was carried out on these compounds to understand the structural features essential for activity. The higher the difference in HOMO and LUMO energy levels the greater was the activity profile. Substitution with fluoro group on the ort Read More

Preventative medicine in the form of vaccination had a huge impact on human health in the 20th Century. Vaccines are now recognized as the most effective line of defence against infectious agents that cause disease and death, and in some cases vaccines have enabled complete eradication of disease from the globe (e.g. smallpox). Nevertheless there are still many human diseases (e.g. viral and parasitic infectio Read More