Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 9, Issue 4, 2009

The 8H-thieno[2,3-b]pyrrolizinones, some of which exert very potent cytotoxic activity against tumor cell lines in vitro, are a promising novel series of anti-cancer agents. These compounds belong to the tripentone family and are based on 9H-pyrrolo[1,2-a]indol- 9-one derivatives and their heterocyclic isosteres. This paper inventories the different synthetic strategies for tripentones and reviews their biological effects and th Read More

Lysophosphatidic acid (LPA) and sphingosine 1-phosphate (S1P) are naturally arising bioactive lipids. The roles of LPA and S1P in angiogenesis, tumor growth and metastasis have recently emerged. Blood platelets are an important source of LPA and S1P in the organism. However, other types of cells including cancer cells expressing autotaxin and sphingosine kinases have the capacity to produce LPA and S1P, respectivel Read More

Natural product extracts are a rich source of small molecules that display antitumor activity. Cantharidin, in the form of the dried body of the Chinese blister beetles: Mylabris phalerata or M. cichorii, displays antitumor activity and induces apoptosis in many types of tumor cells. Cantharidin has been used as an anticancer agent by the Chinese for the treatment of hepatoma and oesophageal carcinoma for a long time. Altho Read More

Isatin (1H-indole-2,3-dione) and its derivatives demonstrate a diverse array of biological and pharmacological activities including anticonvulsant, antibacterial, antifungal, antiviral and anticancer properties. This broad spectrum of biochemical targets has been facilitated by the synthetic versatility of isatin, which has allowed the generation of a large number of structurally diverse derivatives including analogues derived fr Read More

During the last decades multidrug resistance (MDR) emerged as main problem in the anti-cancer therapy with cytostatically active agents. Classical as well as recently developed cytostatics develop the phenomenon of loosing activity in former drug-sensitive cells. Although MDR is a multifactorial process, the main obstacle is the expression of multidrug-efflux pumps that lowers the intracellular drug levels. P-glycoprotein (P-gp) is t Read More

Many cancer cells are known to have defects in the apoptosis machinery. Therefore identification of compounds that can activate or promote apoptosis in cancer cells is an attractive approach for targeted therapies. By applying a novel cell- and caspase-based Anti-cancer Screening Apoptosis Program (ASAP) HTS assay, 4-aryl-4H-chromenes were identified as potent apoptosis inducers. 4- Aryl-4H-chromenes were fo Read More

Omega-3 fatty acids (ω3-FA) were shown to attenuate growth and induce apoptosis in a variety of human cancer cell lines derived from colonic, pancreatic, prostate, and breast cancer. In addition, recent findings indicate that ω3-FA act synergistically with chemotherapeutic agents and may also be used to enhance tumour radiosensitivity. The mechanisms underlying the anti-tumour effects of ω3-FA are complex. Incorporatio Read More

Within the past ten years, a huge volume of research on the synthesis, structure-activity relationships (SAR), and anticancer activities of the urea derivatives was reported. Many aromatic urea derivatives such as N-phenyl-N'-(2-chloroethyl)ureas (CEUs) and benzoylureas (BUs) show good anticancer activity, and these compounds have mainly been proved to be tubulin ligands that inhibit the polymerization of tubulin. Heter Read More