Shixia Feng

Synthesis and evaluation of dihydroartemisinin and dihydroartemisitene acetal dimers showing anticancer and antiprotozoal activity.

Twelve artemisinin acetal dimers were synthesized and tested for antitumor activity in the National Cancer Institute (NCI) in vitro human tumor 60 cell line assay, producing a mean GI(50) concentration between 8.7 (least active) and 0.019 microM (most active). The significant activity of the compounds in this preliminary screen led to additional in vitro antitumor and antiangiogenesis studies. Several active dimers were also evaluated in the in vivo NCI hollow fiber assay followed by a preliminary xenograft study. The title compounds were found to be active against solid tumor-derived cell lines and showed good correlation with other artemisinin-based molecules in the NCI database. The dimers were also evaluated for their antimalarial and antileishmanial activities. The antimalarial activity ranged from 0.3 to 32 nM (IC(50)), compared to 9.9 nM for artemisinin.

Analysis of Flunitrazepam and Its Metabolites in Biological Specimens

Flunitrazepam, 5-(2-fluorophenyl)-1,3-dihydro- l-methyl-7-nitro-2H-1,4-benzodiazepin-2-one, also commonly known as Rohypnol or “roofies,” belongs to a highly potent group of benzodiazepines used mainly as hypnotic, sleeping aid, or preanesthetic agents (1–3). The drug is distributed in 80 countries throughout the world; however, it has never been approved for medicinal use in the United States. It is at present listed as a Schedule IV controlled substance under current U.S. statutes. The drug is smuggled into the United States across the Mexican border or from South American countries through Miami. It is alleged to have been involved in date-rape cases in the 1990s (4–8).