N1-Benzyl Tryptamine Pan-SHIP1/2 Inhibitors: Synthesis and Preliminary Biological Evaluation as Anti-Tumor Agents

Sandra Fernandes, Shea T. Meyer, Jigisha P. Shah, Arijit A. Adhikari, William G. Kerr, John D. Chisholm

Research output: Contribution to journalArticlepeer-review

Abstract

Inhibition of phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase (SHIP) with small molecule inhibitors leads to apoptosis in tumor cells. Inhibitors that target both SHIP1 and SHIP2 (pan-SHIP1/2 inhibitors) may have benefits in these areas since paralog compensation is not possible when both SHIP paralogs are being inhibited. A series of tryptamine-based pan-SHIP1/2 inhibitors have been synthesized and evaluated for their ability to inhibit the SHIP paralogs. The most active compounds were also evaluated for their effects on cancer cell lines.

Original languageEnglish (US)
Article number8451
JournalMolecules
Volume27
Issue number23
DOIs
StatePublished - Dec 2022

Keywords

  • SHIP1
  • SHIP2
  • antitumor
  • medicinal chemistry
  • phosphatase
  • tryptamine

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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