The catalytic, enantioselective, cyclization of phenols with electrophilic sulfenophthalimides onto isolated or conjugated alkenes affords 2,3-disubstituted benzopyrans and benzoxepins. The reaction is catalyzed by a BINAM-based phosphoramide Lewis base catalyst which assists in the highly enantioselective formation of a thiiranium ion intermediate. The influence of nucleophile electron density...

It has been proposed that cytosolic aldehyde dehydrogenase, measured with acetaldehyde as the substrate, is involved in the in vitro and in vivo detoxification of activated cyclophosphamide (CP) metabolites. Higher levels of this enzyme in some normal tissues, such as liver and kidney, are believed to protect these tissues against the toxic effects of CP, whereas relatively lower levels of this...

There are many different chemotherapeutic agents used in cancer treatment. Most of the chemotherapeutic drugs can be divided into alkylating agents, antimetabolites, anthracyclines, plant alkaloids, topoisomerase inhibitors, and other antitumour agents. All of these drugs affect cell division or DNA synthesis and function in some way. Several classes of chemotherapy work by producing a reactive...

Although phosphoramide mustard (PM) is generally recognized as being the most genotoxic metabolite of cyclophosphamide (CP), the contribution of acrolein to the cytogenetic toxicity of CP is unclear. Besides covalently binding to DNA, acrolein can inactivate critical proteins necessary for replicative DNA synthesis, RNA transcription, cell membrane integrity, and metabolism of xenobiotic and en...