Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 6, Issue 3, 2006

The discovery of an inductible form (COX-2) of cyclooxygenases expressed in inflamed tissue lead to the rapid development of selective COX-2 inhibitors [1], denominated coxibs and expected to be useful in the treatment of pathologies such as arthritis without gastrointestinal toxicity compared with non-steroid-antiinflammatory drugs (NSAIDs) which inhibit the gastric mucosal protection assumed by COX-1 isoform [2]. Read More

The biological role of COX-2, the inducible form of cyclooxygenase, is to convert arachidonic acid into prostaglandins (PGs) and thromboxanes (TXs). Overexpressed in many tumors, COX-2 plays a crucial role in cancer through synthesis of PGs which stimulate PGs receptors with subsequent enhancement of cellular proliferation, promotion of angiogenesis, inhibition of apoptosis, stimulation of invasion/motility, and suppressio Read More

Cyclooxygenase-2 (COX-2) overexpression is seen in many malignancies including lung cancer. Elevated tumor prostaglandin E2 (PGE2), a major COX-2 metabolite, levels have been implicated in angiogenesis, tumor growth and invasion, apoptosis resistance and suppression of anti-tumor immunity. Recent studies also revealed that PGE2 signaling may confer cells resistant to targeted growth factor receptor therapy by cro Read More

Breast cancer is the most common cancer among women, and ranks second among cancer deaths in women. Approximately 60% of all breast cancer patients have hormone-dependent breast cancer, which contains estrogen receptors and requires estrogen for tumor growth. Estradiol is biosynthesized from androgens by the cytochrome P450 enzyme complex called aromatase. Aromatase is found in several tissues in th Read More

Non-steroidal anti-inflammatory drugs (NSAIDs), which are known to be cyclooxygenase (COX) inhibitors, have been reported to exert anti-proliferative and pro-apoptotic effects on a variety of cancer cells. Since the COX-2 isoform was found to be overexpressed in a many human cancers, a particular attention was paid on the possible use of selective COX-2 inhibitors in cancer chemoprevention. The present review Read More

Selective inhibition of COX-2 provided a new class of anti-inflammatory, analgesic and antipyretic drugs with significantly reduced side effects and could also be an important strategy for preventing or treating a number of cancers. This review illustrates the molecular modeling methods used for the knowledge of the molecular mechanism of inhibition as well as for the design of selective compounds.

In recent years, clinical applications of recombinantly produced bioactive proteins such as cytokines have attracted attention. However, since these recombinant proteins are rather unstable in vivo, their clinical use as therapeutic agents requires frequent administration at a high dosage. This regimen disrupts homeostasis and results in severe side effects. To overcome these problems, bioactive proteins have been conjugated Read More

Curcumin, a natural component of the rhizome of curcuma longa has emerged as one of the most powerful chemopreventive and anticancer agents. Its biological effects range from antioxidant, anti-inflammatory to inhibition of angiogenesis and is also shown to possess specific antitumoral activity. The molecular mechanism of its varied cellular effects has been studied in some details and it has been shown to ha Read More

Betulinic acid, a pentacyclic triterpene, is widely distributed throughout the tropics. It possesses several biological properties such as anticancer, anti-inflammatory, antiviral, antiseptic, antimalarial, spermicidal, antimicrobial, antileshmanial, antihelmentic and antifeedent activities. However, betulinic acid was highly regarded for its anticancer and anti-HIV activities. Anticancer role of betulinic acid appeared by inducing apopt Read More