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- Title
N1 -Benzyl Tryptamine Pan-SHIP1/2 Inhibitors: Synthesis and Preliminary Biological Evaluation as Anti-Tumor Agents.
- Authors
Fernandes, Sandra; Meyer, Shea T.; Shah, Jigisha P.; Adhikari, Arijit A.; Kerr, William G.; Chisholm, John D.
- 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.
- Subjects
BIOSYNTHESIS; ANTINEOPLASTIC agents; TRYPTAMINE; SMALL molecules; CELL lines
- Publication
Molecules, 2022, Vol 27, Issue 23, p8451
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules27238451