Synthesis and anticancer evaluation of acetylated-lysine conjugated gemcitabine prodrugs.

Gemcitabine is an antimetabolite drug approved for the treatment of various cancers. However, its use is limited due to several issues such as stability, toxicity and drug resistance. Herein, we present the design and synthesis of a series of gemcitabine prodrugs with modifications on the 4--amino group by employing an acetylated l- or d-lysine moiety masked by different substitutions.

Investigation of chetomin as a lead compound and its biosynthetic pathway.

Chaetomium fungi produce a diversity of bioactive compounds. Chaetomium cochliodes SD-280 possesses 91 secondary metabolite gene clusters and exhibits strong antibacterial activity. One of the active compounds responsible for that activity, chetomin, has a minimum inhibitory concentration (MIC) for anti-methicillin-resistant Staphylococcus aureus (MRSA) of 0.

Transition-metal-free KI-catalyzed regioselective sulfenylation of 4-anilinocoumarins using Bunte salts.

An efficient and eco-friendly protocol for the KI-catalyzed regioselective sulfenylation of 4-anilinocoumarins with Bunte salts was established. The reaction worked smoothly under metal-free conditions and afforded a wide range of sulfenylated 4-anilinocoumarins with potential bioactivity in moderate to excellent yields. This method would expand the still limited scope of synthesis methods for C-S bond formation using Bunte salts.