Photo of Xiangshu Xiao, Ph.D.

Xiangshu Xiao Ph.D.

  •      (503) 494-4748
    • Professor of Chemical Physiology and Biochemistry School of Medicine
    • Cancer Biology Graduate Program School of Medicine
    • Graduate Program in Biomedical Sciences School of Medicine

Our research is at the emerging interface of chemistry and biology by using chemical tools to dissect the signaling pathways implicated in cancer development and maintenance. A particular focus in the lab is to develop chemical tools and potential cancer therapeutics for targets that are not well understood. Synopses of two ongoing projects are listed below:

Areas of interest

  • Chemical biology, organic synthesis, medicinal chemistry
  • target identification of bioactive molecules


  • B.S., Beijing Medical University, Beijing China 1998
  • M.S., Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai China 2001
  • Ph.D., Purdue University, West Lafayette Indiana 2005
  • Fellowship:

    • Postdoc 2007, UT Southwestern Medical Center, Dallas, TX

Memberships and associations

  • American Chemical Society,


  • "An efficient and selective method for hydrolysis of acetonides" Synlett  2001
  • "Isolation and characterization of coactivator-binding peptoids from a combinatorial library" Molecular BioSystems  2006
  • "Synthesis of 14,15-EET from Arachidonic Acid Using Urea-Hydrogen Peroxide as the Oxidant" Synthetic Communications January 2 2015
  • "A cell-permeable synthetic transcription factor mimic" Angewandte Chemie - International Edition  2007
  • "Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines" Bioorganic and Medicinal Chemistry Letters June 2 2005
  • "Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids" Journal of Medicinal Chemistry July 17 2003
  • "The unexpected reductive products of δ- alkoxyenal by sodium borohydride in methanol with a trace of magnesium methoxide" Chinese Chemical Letters September 2002
  • "Targeting CREB for cancer therapy" Current Cancer Drug Targets  2010
  • "An ab initio quantum mechanics calculation that correlates with ligand orientation and DNA cleavage site selectivity in camptothecin-DNA-topoisomerase I ternary cleavage complexes" Journal of the American Chemical Society July 20 2005
  • "Design, synthesis, and biological evaluation of cytotoxic 11-aminoalkenylindenoisoquinoline and 11-diaminoalkenylindenoisoquinoline topoisomerase I inhibitors" Bioorganic and Medicinal Chemistry October 1 2004
  • "On the mechanism of conversion of 4-carboxy-3,4-dihydro-3-phenyl-1(2H)-isoquinolones to indeno[1,2-c]isoquinolines by thionyl chloride" Tetrahedron October 9 2006
  • "Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity" Journal of Medicinal Chemistry June 25 2015
  • "Structure-activity relationship studies of naphthol AS-E and its derivatives as anticancer agents by inhibiting CREB-mediated gene transcription" Bioorganic and Medicinal Chemistry December 1 2012
  • "Synthesis and evaluation of an O-Aminated naphthol AS-E as a prodrug of CREB-mediated gene transcription inhibition" Letters in Organic Chemistry June 2013
  • "Synthesis of a sec-precursor and analogues of macrolactin A" Chemistry Letters July 5 2005
  • "Novel type of prodrug activation through a long-range O,N-acyl transfer" ACS Medicinal Chemistry Letters October 9 2014
  • "Soluble epoxide hydrolase dimerization is required for hydrolase activity" Journal of Biological Chemistry March 15 2013
  • "Synthesis, crystal structure, and conversion of the polycyclic tris-anhydrotetramer of O-aminobenzaldehyde to Cu(TAAB)2+" Synthetic Communications  2004
  • "Discovery of a potent anti-tumor agent through regioselective mono-N-acylation of 7H-pyrrolo[3,2-f]quinazoline-1,3-diamine" MedChemComm  2013
  • "The chemistry and pharmacology of privileged pyrroloquinazolines" MedChemComm April 1 2015
  • "Erratum" MedChemComm  2014
  • "Effect of E-ring modifications in camptothecin on topoisomerase I inhibition" Journal of Organic Chemistry November 11 2005
  • "A facile method to transform trans-4-carboxy-3,4-dihydro-3-phenyl-1(2H)- isoquinolones to indeno[1,2-c]isoquinolines" Journal of Organic Chemistry August 5 2005
  • "Design and synthesis of a cell-permeable synthetic transcription factor mimic" ACS Combinatorial Science July 2007
  • "Design, Synthesis, and Biological Evaluation of Indenoisoquinoline Topoisomerase I Inhibitors Featuring Polyamine Side Chains on the Lactam Nitrogen" Journal of Medicinal Chemistry December 18 2003
  • "On the binding of indeno[1,2-c]isoquinolines in the DNA-topoisomerase I cleavage complex" Journal of Medicinal Chemistry May 5 2005
  • "Rapid identification of improved protein ligands using peptoid microarrays" Bioorganic and Medicinal Chemistry Letters July 15 2009
  • "Total synthesis and biological evaluation of 22-hydroxyacuminatine" Journal of Medicinal Chemistry February 23 2006
  • "Design, synthesis, and biological evaluation of conformationally constrained analogues of naphthol AS-E as inhibitors of CREB-mediated gene transcription" Journal of Medicinal Chemistry April 26 2012
  • "Novel autoxidative cleavage reaction of 9-fluoredenes discovered during synthesis of a potential DNA-threading indenoisoquinoline" Journal of Organic Chemistry October 29 2004

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