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Synthesis and biological evaluation of analogs of altohyrtin C (spongistatin 2) |
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| Authors: | Carl E Wagner Qiang Wang Craig R Fairchild Clayton H Heathcock |
| Institution: | a Arizona State University at the West Campus, Department of Integrated Natural Sciences, Glendale, AZ 85306, United States b Chemocentryx, Inc, Mountain View, CA 94043, United States c Bristol-Myers Squibb Co., Oncology Drug Discovery, Princeton, NJ 08534, United States d Center for New Directions in Organic Synthesis, Department of Chemistry, University of California, Berkeley, CA 94720, United States |
| Abstract: | Several structural analogs that contain only part of the altohyrtin structure have been prepared and compared with synthetic altohyrtin C (2) for in vitro cytotoxicity against human colon (HCT116) and ovarian (A2780) cell lines. Whereas altohyrtin C was found to be exceedingly potent against these lines (IC50=0.0003 μM), analogs 3-5 were >27,000-fold less potent (IC50>8 μM). Analogs 6 and 7 also demonstrated weak cytotoxicity with IC50 values for the HCT116 and A2780 cells of 4.8 μM and 2.4 μM, respectively, for 6. |
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