Current Topics in Medicinal Chemistry - Volume 16, Issue 22, 2016

Telomeres are the terminal part of the chromosome containing a long repetitive and noncodifying sequence that has as function protecting the chromosomes. In normal cells, telomeres lost part of such repetitive sequence in each mitosis, until telomeres reach a critical point, triggering at that time senescence and cell death. However, in most of tumor cells in each cell division a part of the telomere is lost, however the app Read More

Histone deacetylases (HDACs) regulate gene expression by modulating chromatin architecture via histone hypoacetylation. They play a key role in regulating cellular processes including cell cycle arrest and apoptosis. Hyperactivity of HDACs plays a key role in tumour onset and progression making these enzymes as striking targets for anticancer drugs and therapy. Certain cancers are associated with upregulation of specific Read More

Background: Aberrant signal transducer and activator of transcription 3 (STAT-3) molecular signaling elicit hepatocellular carcinoma (HCC) in humans. Therefore, targeting STAT-3 is considered as an attractive option towards suppression of HCC in humans. Objective: Our objective is to identify a potential small molecule inhibitor that can specifically target STAT-3 and suppress HCC. Methods: In this study, we analyze a gr Read More

Nitroxyl (HNO), the one electron reduced form of nitric oxide (NO), shows a very distinct chemistry and biology from that of NO. Chemical profile is characterized by reactions with thiols and thiol proteins such as aldehyde dehydrogenase, glyceraldehyde 3-phosphate dehydrogenase, caspases among others. Biological profile of HNO includes cardioprotective actions especially in cases of heart failure. This short review focuses o Read More

Research over the years has gradually and sequentially highlighted contributory role of hypothalamic- based kisspeptin-signaling axis as a major positive modulator of the neuroendocrinological reproductive axis in mammals. However, a series of landmark studies provided convincing evidence of role of this signaling in regulation of cancer development and progression. It is becoming progressively more understandabl Read More

Cancer is a multifaceted and genomically complex disease. Rapidly accumulating preclinical and clinical studies are emphasizing on wide ranging molecular mechanisms that underpin cancer development, progression and metastasis. Intratumor heterogeneity, loss of apoptosis, rapidly developing resistance against molecular therapeutics and off-target effects are some of the deeply studied resistance mechanisms. Dat Read More

A major impediment for cancer chemotherapy is the development of multidrug-resistance (MDR). Continuous use of chemotherapeutic drugs during cancer therapy induces the expression of PGlycoprotein (P-gp, MDR1), an ATP dependant transporter, which in turn reduces the intracellular accumulation of chemotherapeutic drugs leading to MDR. Extensive research over the years has identified several potential P-gp inhibito Read More

In the present study an efficient strategy for the synthesis of thiazole and thiadiazole derivatives was developed and clubbed together both of the substituted nucleus to form the analogues of combretastatin A-4 (tubulin polymerization inhibitors.). Synthesis was started by the reaction of substituted benzoic acid with thionyl chloride followed by the reaction with hydrazine, p-chloro benzaldehyde and thioglycolic acid to for Read More