Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 17, Issue 12, 2017

Cancers have increased threat to human health due to the limited treatment efficacy of chemotherapy and radiotherapy with a series of toxicity and side effects; therefore, the development and utilization of natural products with potential preventive and therapeutic efficacy, and less toxicity and side effects will be beneficial to promote the health of cancer patients. In this article, the activity of ampelopsin as a natural flavonoi Read More

Cancer cells do create hostile microenvironment (deprivation of nutrients, accumulation of acidity, anoxic habitat). Those cells are not only adapted to this sanctuary environment, blunting of immunity but also, grow, migrate to the distal area (metastasis) and communicate with each other in a unique population structure and organization too (clonal expansion). The adaptation requirements push those types of adaptable cells (c Read More

Background: Rhein (1,8-dihydroxy-3-carboxyanthraquinone) is a monomer of anthraquinone derivatives mainly found in Polygonaceae plants such as Rhubarb, and Cuspidatum, widely used in the traditional Chinese medicine with many pharmacological activities, such as antitumor, anti-inflammatory and antifibrotic effects, and regulation of glucose and lipid metabolism. Objective: To conclude the role of Rhein in cancer Read More

Background: Renal cell carcinoma (RCC) is responsible for 4% of all neoplasms in adults and 80% of all primary renal tumours. In the European Union, there are almost 84000 new cases and 35000 deaths each year due to RCC. In the last five decades, patients with localised RCC will develop recurrence of disease after nephrectomy in about 50% of cases. Considering the number of novel targeted therapies approved in the la Read More

Background: One of the promising scaffolds in drug discovery is the fused pyrimidine derivatives. Objective and Method: Efficient synthesis of a novel series of 18 new 1,8-naphthyridine-3-carbonitrile, 2-amino pyrido[2,3-d]pyrimidine derivatives via multi-component reactions of aromatic aldehydes, active methylene, and an aromatic amine under microwave irradiation and evaluation of their anticancer activity and possibl Read More

Background: Berberine, a quaternary ammonium salt from the protoberberine group of benzylisoquinoline alkaloids has drawn high attention for its several biological potencies. Objective: To furnish new rationalized derivatives based on berberine core which can deliver promising antioxidant and cytotoxic activities. Method: The N-Mannich base of an isoquinoline alkaloid, berberine, bearing substituted benzothiazole moieties was o Read More

Background: Poly(hydroxyalkanoates) (PHA) have recently attracted increasing attention due to their biodegradability and high biocompatibility, which makes them suitable for the development of new prolong drug formulations. Objective: A preclinical toxicology study of paclitaxel biopolymer formulation (PBF) (paclitaxel-loaded poly(3- hydroxybutyrate) (PHB) microparticles) was done in order to assess its safety and to forecas Read More

Background: Excessive reactive species derived from oxygen and nitrogen leads to oxidative damage to tissue and organs. Capsaicin (CAP), a pungent component found in red pepper can prevent oxidative stress. Objective: The aim of the present work was to evaluate the protective effects of CAP loaded nano-emulsomes (EML) against the oxidative stress of rat livers induced through sodium fluoride (NaF). Method: E Read More

Background: Recently, we devoted to disclosing the antibacterial activities of enmein-type 6,7-seco-ent-kauranoid derivatives. Objective: Eleven new enmein-type diterpenoid derivatives with different substituents and drug-like properties were designed and synthesized. Method: The antimicrobial activities against E. coli, S. aureus, B. subtilis and M. albicans were disclosed. The antiproliferative activities against human Read More

Background: Cell migration is an essential process for survival and differentiation of mammalian cells. Numerous diseases are induced or influenced by inappropriate regulation of cell migration, which plays a key role in cancer cell metastasis. In fact, very few anti-metastasis drugs are available on the market. SphKs are enzymes that convert sphingosine to sphingosine-1-phosphate (S1P) and are known to control variou Read More

Background: HMGB1 (High Mobility Group Box-1) is a very versatile highly abundant architectural protein that plays multiple roles in human health and diseases. Under physiological condition it serves as an amazing assortment of roles in different compartments of cell. The reported high expression of HMGB1 in almost all types of human cancers and inflammatory diseases makes it a critical molecular therapeutic target. Read More

Background: Phenolic compounds are known for their cytotoxic properties against cancer cells despite their still unclear general mechanism of action. Herein is reported the evaluation of the cytotoxic effects of on human osteosarcoma cells of nine phenol derivatives against osteosarcoma cells, and some insights on their mechanism. Method and Results: The cytotoxicity was characterized by cell viability, scratch assay, cell Read More

Background: Ovarian cancer is most lethal among all gynecologic malignancies. Paclitaxel (PTX) is well used chemotherapeutic regimen for cancer control; however its undesired toxicity has been a matter of concern for clinicians. Here, we used the graphene oxide coated nanotised apigenin (GO-NA) to enhance the efficacy of paclitaxel. Objective: The combined use of paclitaxel (PTX) and nanotised apigenin (NA) may reduce Read More