β-Amino alcohols are versatile intermediates in the synthesis of various biologically potent compounds, which can also be achieved by ring opening of epoxides by amines. In the present review, focus has been placed on the ring opening of epoxides with amines under a variety of reaction parameters reported during 2011–2015. All the factors that resulted in excellent yields and high regioselectivity, are environmentally benign, and use mild conditions have been discussed in detail. In addition, the applications of these methods in the synthesis of biologically active compounds such as β-blockers have also been described.
1 February 2010 in European Journal of Medicinal Chemistry
Cancer is a serious threat to human beings and is the second-largest cause of death all over the globe. Chemotherapy is one of the most common treatments for cancer; however, drug resistance and severe adverse effects are major problems associated with anticancer therapy. New compounds with multi-target inhibitory properties are targeted to surmount these challenges. Cyclooxygenase-2 (COX-2) is overexpressed in cancers of the pancreas, breast, colorectal, stomach, and lung carcinoma. Therefore, COX-2 is considered a significant target for the synthesis of new anticancer agents. This review discusses the biological activity of recently prepared dual anticancer and COX-2 inhibitory agents. The most important intermolecular interactions with the COX-2 enzyme have also been presented. Analysis of these agents in the active area of the COX-2 enzyme could guide the introduction of new lead compounds with extreme selectivity and minor side effects.