Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 16, Issue 3, 2016

Heat shock protein 90 (Hsp90) is an important member of the chaperone protein family and it is involved in stabilization, regulation, and maintenance of oncogenic client proteins with co-chaperones. Cochaperones regulate the ATPase activity of Hsp90 and its interactions with oncogenic client proteins. Therefore, Hsp90 and its co-chaperones have become significant therapeutic targets for cancer treatment. M Read More

The continuous activation of the mitogen-activated protein kinase signaling cascade, typified by the BRAFV600E mutation, is one of the key alterations in melanoma. Accordingly, two BRAF inhibitors (BRAFi), vemurafenib and dabrafenib are utilized to treat melanoma and resulted in an excellent clinical outcome. However, the clinical success is not long-lasting, and the BRAFi resistance and disease progression inevitably Read More

Core-shell structured aggregates of amphiphilic block copolymer are hopefully drug delivery system because of their ability to encapsulate hydrophobic drugs, and their hydrophilic shell can prolong retention time of drugs in the blood circulation system. Cyclodextrin is a kind of hydrophilic polysaccharide containing multiple hydroxyl groups, providing an inner hole that can load small molecule through host-guest Read More

The hedgehog (Hh) signaling pathway, which is almost completely silenced in normal adult tissues but highly activated in cancer, offers ideal drug targets for small molecule development. During the last few years, several studies have indicated that the Hh pathway plays a role in tumor development and maintenance, and novel drugs inhibiting Hh signaling have been discovered. Although results from clinical trials in pati Read More

Although surgical resection is the standard curative therapy for gastric cancer, these tumors are often diagnosed at an advanced stage, when surgery is not recommended. Alternative treatments such as radiotherapy and chemotherapy achieve only very modest results. There is therefore an urgent need to advance in this field of oncologic gastroenterology. The poor response of gastric cancer to chemotherapy is usually d Read More

The phosphorus-containing glycerolipid based antitumor drugs (edelfosine as a prototype) are currently in clinical trials. To avoid the use of potentially harmful phosphoric reagents in the preparation of biologically active glycerolipids, and to obtain the compounds without the phosphoester bond cleavable inside the cells, we developed the synthesis of non-phosphorous glycerolipids (NPGLs) with neutral or catio Read More

Angiogenesis is the process of new blood vessel formation, regulated by a number of pro- and antiangiogenic factors and usually begins in response to hypoxia. Exogenous administration of melatonin has shown numerous anti-tumor effects and appears to inhibit tumor angiogenesis. However, many factors involved in the anti-angiogenic effect of melatonin are still under investigation. Here, we evaluate the effects of Read More

In vitro antitumor activity of various organogallium(III) complexes (1–8) has been tested against CT26CL25, HCT116, SW480 colon cancer cell lines. CV and MTT assays were used to assess on the antiproliferative effect of investigated organogallium(III) complexes. From the investigated complexes, the most active was found to be tetranuclear compound 8 against CT26CL25 cells. Flow cytometric analysis of the CT26CL2 Read More

In an attempt to improve the localized paclitaxel delivery, carrier based thermoresponsive chitosan hydrogel was exploited in the present study. Nanoliposomes as carrier for paclitaxel were prepared and optimized in strength of 6 mg/ml similar to marketed paclitaxel formulation. The chitosan solution (2% w/v) mixed with different concentrations of dibasic sodium phosphate (DSP) was evaluated as thermoresponsive s Read More

Twenty-four new dibenzo[b,d]furan–1H-1,2,4-triazole derivatives were synthesized and investigated for in vitro cytotoxic activity against five tumor cell lines. The results show that the substitution at 4-position of the 1,2,4-triazole with a benzyl, 4-bromophenacyl or naphthylacyl group could be crucial for prommoting cytotoxic activity. Especially, compound 28 was found to be the most powerful derivative with IC50 values lower t Read More

Background and Aim: The incidence of acute lymphoblastic leukemia (ALL) is highest in childhood malignant tumor in China. The high-dose methotrexate (HDMTX) treatment is very effective in ALL, and it can improve event-free survival rate. However, while executing the anti-tumor effect, it produces highly toxic effects on rapidly dividing cells which are normal. It seems probable that the HDMTX treatment injures int Read More

Purpose: Cisplatin as a platinum (Pt)-based chemotherapeutic compound is commonly applied for the treatment of several types of cancer. Nonetheless, drug resistance and severe adverse effects have been observed upon using cisplatin. Here, we have explored the cytotoxicity of novel Pt-based compounds on several cancer cell lines. Methods: Five synthetic Pt compounds as well as cisplatin were investigated by XTT as Read More