The β-lactam (4-membered cyclic amide) scaffold is primarily the most important class of antibiotics, among various classes of pharmacophores, due to their diverse and interesting antimicrobial properties. However, the versatility of the β-lactam core structure, combined with the innovation of medicinal chemists, has repeatedly led to the development of new generations of β-lactam antibiotics that are capable of overcoming the complications caused by mounting bacterial resistance. Other than anti-infective properties β-lactam derivatives also demonstrated a wide range of medicinal activity which includes, but are not limited to, antidiabetic, anti-inflammatory, antiparkinsonian, anti-HIV as well as anticancer. Research related to anticancer β-lactams is comparatively new and this area of drug discovery research has not been explored in detail. It has been found that ribonucleotide reductase, thymidylate synthase, thymidylate phosphorylase, topoisomerase II, phosphatase 2A, β-tubulin, aminopeptidase N, cytidine deaminase are the proteins that play pivotal role at the various stages of cell proliferation, invasion, metathesis and angiogenesis; hence responsible for the propagation of cancer. As a part of our ongoing investigation to develop new and novel small molecule inhibitors, we have designed and synthesized a series of β-lactams as novel anticancer agents. Staudinger [2+2] ketene-imine cycloaddition reaction has been used as one of the major steps to achieve the target β-lactams in good yield.

β-Lactams as anticancer agent: Design, synthesis, and biological evaluation

251st National Meeting (2016)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.