Synthesis of kurasoin B analogs
Kurasoin B (1), isolated in 1996 by Uchida et al, selectively inhibits Farnesyltransferase (FTase), an enzyme responsible for activating human RAS proteins (ref. 1). When RAS proteins are mutated and then activated, they contribute 20 to 30 percent of all human tumors, including those of the pancreas, colon, small intestine, lung, prostate, liver, skin, and thyroid, as well as multiple myeloma and a number of leukemias (ref. 2). Kurasoin B, therefore, has great potential as a cancer drug lead.
Nielson, J. R.; Christiansen, M. A.; Andrus, M. B. “Synthesis of kurasoin B analogs.” Abstracts of Papers, 236th ACS National Meeting, Salt Lake City, UT, United States, April 22-26, 2009. Poster.