Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 12, Issue 9, 2012

NR4A1 (Nur77), NR4A2 (Nurr1) and NR4A3 (Nor-1) are three members of the orphan nuclear receptor (NR) family referred to as NR4A family. This subgroup activates gene expression in a constitutive ligand-independent manner. These nuclear receptors are classified as early response genes that are induced by a diverse range of signals. These orphan NRs have been implicated in cell cycle regulation, apoptosis, inflammation, Read More

Multidrug resistance (MDR) is a limiting step on the success of cancer chemotherapy. The drug efflux mediated by P-gp (Pglycoprotein) is one of the best studied mechanisms of MDR. This paper focuses on the inhibitory P-gp efflux activity, pharmacophore modeling and structure-activity relationships studies of sixteen macrocyclic diterpenes and polycyclic derivatives obtained from Euphorbia species. The MDR human col Read More

Peroxisome Proliferator-Activated Receptor-γ (PPARγ) is an extensively studied ligand-activated nuclear hormone receptor that functions as transcription factor and plays an important role in diverse biological processes, such as lipid metabolism and insulin sensitization. Recent studies have demonstrated that PPARγ is over-expressed in many tumor types, including breast cancer, suggesting a possible role in tumor dev Read More

Extensive evidence implicates CCR5 and its ligands in the biology of tumors, although there is considerable controversy regarding the role of this chemokine receptor in cancer progression. The discrepancies between the pro- and anti-tumor effects of CCR5 might derive from its expression by cell types with opposing functions in tumor progression and the context in which tumors originate. We propose that CCR5 is necessary fo Read More

Doxorubicin, one of the most effective anticancer drugs currently known, is commonly used against breast cancer. However, its clinical use is restricted by dose-dependent toxicity (myelosuppression and cardiotoxicity), the emergence of multidrug resistance and its low specificity against cancer cells. Nanotechnology is a promising alternative to overcome these limitations in cancer therapy as it has been shown to reduce Read More

Our previous studies showed that zinc (II), cadmium (II) and nickel (II) complexes with 2-formylpyridine selenosemicarbazone induce apoptosis in cancer cells via activation of mitochondrial pathway. Herein, we reported their antimetastatic properties. Nickel (II), and zinc (II) complexes exhibited the strongest inhibitory potential towards MMP-2/9, while all investigated compounds significantly decreased proteolytic activit Read More

The treatment of advanced urothelial cancer of the bladder has evolved substantially during recent years. Chemotherapy has been the mainstay of treatment and confers survival advantage. Despite such advances, the chemotherapy of bladder cancer is far from satisfactory due to severe side effects. Targeted therapy with novel drugs directed at specific molecular pathways opens promising new avenues to improve patient out Read More

Hepatocellular carcinoma (HCC) is one of the hard-treating and high mortality cancers for which novel therapies are very much in need. Sorafenib is the first medication that is now approved for the treatment of patients with advanced HCC [1]. Sorafenib is a multikinase inhibitor targeting the Raf serine/ threonine kinases and the VEGFR1-3, PDGFR-b, c-Kit, Flt3 and p38 tyrosine kinases [1]. Here, an in silico approach was direct Read More

An activating mutation (V617F) in the pseudokinase domain of the Janus kinase (JAK)-2 tyrosine kinase has been described in 90% of patients with polycythemia vera (PV) and 50% of patients with essential thrombocythemia (ET) and primary myelofibrosis (MF). The discovery of JAK2V617F stirred the development of JAK2 inhibitors for treatment of patients with MF, ET and PV. Similar to other tyrosine kinase (TK) inhibitors in Read More

Head and neck cancer is the sixth large type of cancer in the world. The treatment regimens for head and neck cancer encompass surgery, radiotherapy and chemotherapy. However, all current treatment regimens for head and neck cancer have adverse effects. Therefore, continuing investigations have been undertaken to seek less toxic therapies to reduce treatment morbidity for head and neck cancer. Substantial e Read More

The indolo[2,3-a]carbazole alkaloids constitute an important class of natural products with interesting and diverse biological activities. A series of novel ring-fused indolocarbazoles were synthesized and evaluated for inhibition of topoisomerase I-mediated relaxation of supercoiled DNA and in vitro antitumor activity. The derivatives bearing a methylenedioxy or an ethylenedioxy ring fused onto the nonglycosylated indole (1a, 1b Read More

Sulforaphane (SFN), one of naturally occurring isothiocyanates (ITCs), has huge cancer chemopreventive potential. It modulates cell death, cell cycle, angiogenesis, susceptibility to carcinogens, invasion and metastasis and possesses antioxidant activities. It functions as an inhibitor of phase I enzymes and also as an inducer of phase II detoxification enzymes through different ways. NF-E2- related factor-2(Nrf-2), as well as mito Read More

Structure-based modeling combined with rational drug design, and high throughput screening approaches offer significant potential for identifying and developing lead compounds with therapeutic potential. The present review focuses on these two approaches using explicit examples based on specific derivatives of Gossypol generated through rational design and applications of a cancer-specificpromoter derived from Progressi Read More