Communication

Structural Determination of NSC 670224, Synthesis of Analogues and Biological Evaluation

  1. Nathaniel B. Zuckerman1,
  2. Andrew S. Myers1,
  3. Dr. Tiffani K. Quan2,3,
  4. Walter M. Bray1,
  5. Prof. R. Scott Lokey1,
  6. Prof. Grant A. Hartzog2,
  7. Prof. Joseph P. Konopelski1,*

Article first published online: 29 FEB 2012

DOI: 10.1002/cmdc.201200038

Issue

ChemMedChem

ChemMedChem

Volume 7, Issue 5, pages 761–765, May 2012

Additional Information

How to Cite

Zuckerman, N. B., Myers, A. S., Quan, T. K., Bray, W. M., Lokey, R. S., Hartzog, G. A. and Konopelski, J. P. (2012), Structural Determination of NSC 670224, Synthesis of Analogues and Biological Evaluation. ChemMedChem, 7: 761–765. doi: 10.1002/cmdc.201200038

Author Information

  1. 1

    Department of Chemistry and Biochemistry, University of California, Santa Cruz (UCSC), PSB 230, 1156 High Street, Santa Cruz, CA 95064 (USA)

  2. 2

    Department of Molecular, Cell and Developmental Biology, University of California, Santa Cruz (UCSC), Sinsheimer Labs, 1156 High Street, Santa Cruz, CA 95064 (USA)

  3. 3

    Department of Biochemistry and Biophysics, University of California, San Francisco (UCSF), Genentech Hall, MC 2140600, 600 16th Street, Suite S222, San Francisco, CA 94158 (USA)

*Department of Chemistry and Biochemistry, University of California, Santa Cruz (UCSC), PSB 230, 1156 High Street, Santa Cruz, CA 95064 (USA)

Publication History

  1. Issue published online: 25 APR 2012
  2. Article first published online: 29 FEB 2012
  3. Manuscript Received: 18 JAN 2012

Funded by

  • US National Institutes of Health. Grant Number: 5R01GM084530-08
  • University of California, Santa Cruz (USA)

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Keywords:

  • affinity probes;
  • drug discovery;
  • high-throughput screening;
  • medicinal chemistry;
  • tamoxifen
Thumbnail image of graphical abstract

Follow my lead! NSC 670224, previously shown to be toxic to Saccharomyces cerevisiae at low micromolar concentrations, potentially acts via a mechanism of action related to that of tamoxifen (NSC 180973), breast cancer drug. The structure of NSC 670224, previously thought to be a 2,4-dichloro arene, was established as the 3,4-dichloro arene, and a focused library of analogues were synthesized and biologically evaluated.

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