enzyme inhibitors Archives

Improving the effectiveness of an anticancer fluoropyrimidine by molecular hybridisation

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Dr Kalman redesigned the anticancer drug capecitabine (Cape)to resist metabolic conversion to 5-fluorouracil and thereby prevent its associated potentially fatal toxicities.

Capecitabine (Cape) – a fluoropyrimidine used primarily in the treatment of breast and colorectal cancer – disrupts the synthesis of DNA in cancer cells following its conversion to 5-fluorouracil (FU). Since FU has been associated with several potentially fatal side effects, Dr Thomas I. Kalman at the University at Buffalo and The State University of New York has developed a […]

Fragment-based design of isoquinoline derivatives as anti-inflammatory drugs

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Dr Masakazu Atobe and his colleagues have developed a methodology that can be applied to the discovery of effective drugs.

Fragment-based drug discovery (FBDD) is a well-established high-throughput screening method for drug generation. Fragment molecules used in FBDD tend to be structurally less complex than the compounds used in conventional high-throughput screening techniques. Dr Masakazu Atobe from Asahi Kasei Pharma Corporation in Japan and his colleagues have developed a methodology that can be applied to the discovery of effective drugs […]