Synthesis and biological evaluation of analogs of altohyrtin C (spongistatin 2)

Carl Wagner, Qiang Wang, Alexander Melamed, Craig R. Fairchild, Robert Wild, Clayton H. Heathcock

Research output: Contribution to journalArticle

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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.

Original languageEnglish (US)
Pages (from-to)124-136
Number of pages13
JournalTetrahedron
Volume64
Issue number1
DOIs
StatePublished - Jan 1 2008

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Cytotoxicity
Inhibitory Concentration 50
HCT116 Cells
Cells
Colon
Cell Line
altohyrtin C

ASJC Scopus subject areas

  • Biochemistry
  • Organic Chemistry
  • Drug Discovery

Cite this

Wagner, C., Wang, Q., Melamed, A., Fairchild, C. R., Wild, R., & Heathcock, C. H. (2008). Synthesis and biological evaluation of analogs of altohyrtin C (spongistatin 2). Tetrahedron, 64(1), 124-136. https://doi.org/10.1016/j.tet.2007.10.065

Synthesis and biological evaluation of analogs of altohyrtin C (spongistatin 2). / Wagner, Carl; Wang, Qiang; Melamed, Alexander; Fairchild, Craig R.; Wild, Robert; Heathcock, Clayton H.

In: Tetrahedron, Vol. 64, No. 1, 01.01.2008, p. 124-136.

Research output: Contribution to journalArticle

Wagner, C, Wang, Q, Melamed, A, Fairchild, CR, Wild, R & Heathcock, CH 2008, 'Synthesis and biological evaluation of analogs of altohyrtin C (spongistatin 2)', Tetrahedron, vol. 64, no. 1, pp. 124-136. https://doi.org/10.1016/j.tet.2007.10.065
Wagner, Carl ; Wang, Qiang ; Melamed, Alexander ; Fairchild, Craig R. ; Wild, Robert ; Heathcock, Clayton H. / Synthesis and biological evaluation of analogs of altohyrtin C (spongistatin 2). In: Tetrahedron. 2008 ; Vol. 64, No. 1. pp. 124-136.
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