Pyran is an oxygen-containing heterocyclic moiety, which exhibits an array of pharmacological properties. Pyran is also one of the important structural subunits found widely in natural products, e.g. coumarins, benzopyrans, sugars, flavonoids, xanthones, etc. The diverse anticancer capabilities of pyrans have been additionally evidenced by the fact that this heterocycle has recently been a focal point for researchers worldwide. This review provides a summary of pyran-based anticancer compounds, with emphasis on the past 10 years. It focuses on advancements in the field of naturally occurring pyrans as anticancer agents. The discussion also includes structure–activity relationships, along with the structures of the most promising molecules, their biological activities against several human cancer cell lines, as well as mechanistic insights discovered through the pharmacological evaluation and molecular modeling of pyran-based molecules. The promising activities revealed by these pyran-based scaffolds undoubtedly place them at the forefront for the discovery of prospective drug candidates. Thus, they could therefore be of great interest to researchers working on the synthesis of antitumour drug candidates.
Background: The most recurrent and considered second most frequent cause of cancer-related deaths worldwide in women is the breast cancer. The key to diagnosis is early prediction and a curable stage but still treatment remains a great clinical challenge. Origin of the Problem: A number of studies have been carried out for the treatment of breast cancer which includes the targeted therapies and increased survival rates in women. Essential PI3K/mTOR signaling pathway activation has been observed in most breast cancers. The cell growth and tumor development in such cases involve phosphoinositide 3 kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) complex intracellular pathway. Hypothesis: Through preclinical and clinical trials, it has been observed that there are a number of other inhibitors of PI3K/Akt/mTOR pathway, which either alone or in combination with cytotoxic agents can be used for endocrine therapies. Conclusion: Structure and regulation/deregulation of mTOR provides a greater insight into the action mechanism. Also, through this review, one could easily scan first and second generation inhibitors for PI3K/Akt/mTOR pathway besides targeted therapies for breast cancer and the precise role of mTOR.
31 July 2013 in Mini-Reviews in Medicinal Chemistry
Imidazoles are one of the most promising and vigorously pursued areas of contemporary antifungal chemotherapy depicting broad spectrum and potent activity. They have relatively simple molecular nucleus, which is amenable to many structural modifications. These agents have several favorable properties such as excellent bioavailability, good tissue penetrability and permeability and a relatively low incidence of adverse and toxic effects. They have been found effective in the treatment of various infectious diseases. This paper is an attempt to review the therapeutic potential of imidazoles as antifungal with an updated account on their development.
1 January 2017 in Oxidative Medicine and Cellular Longevity
Depression is a serious disorder that affects hundreds of millions of people around the world and causes poor quality of life, problem behaviors, and limitations in activities of daily living. Therefore, the search for new therapeutic options is of high interest and growth. Research on the relationship between depression and oxidative stress has shown important biochemical aspects in the development of this disease. Flavonoids are a class of natural products that exhibit several pharmacological properties, including antidepressant‐like activity, and affects various physiological and biochemical functions in the body. Studies show the clinical potential of antioxidant flavonoids in treating depressive disorders and strongly suggest that these natural products are interesting prototype compounds in the study of new antidepressant drugs. So, this review will summarize the chemical and pharmacological perspectives related to the discovery of flavonoids with antidepressant activity. The mechanisms of action of these compounds are also discussed, including their actions on oxidative stress relating to depression.