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

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 SHI...

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Autores principales: Fernandes, Sandra, Meyer, Shea T., Shah, Jigisha P., Adhikari, Arijit A., Kerr, William G., Chisholm, John D.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9738565/
https://www.ncbi.nlm.nih.gov/pubmed/36500543
http://dx.doi.org/10.3390/molecules27238451
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author Fernandes, Sandra
Meyer, Shea T.
Shah, Jigisha P.
Adhikari, Arijit A.
Kerr, William G.
Chisholm, John D.
author_facet Fernandes, Sandra
Meyer, Shea T.
Shah, Jigisha P.
Adhikari, Arijit A.
Kerr, William G.
Chisholm, John D.
author_sort Fernandes, Sandra
collection PubMed
description 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.
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spelling pubmed-97385652022-12-11 N1-Benzyl Tryptamine Pan-SHIP1/2 Inhibitors: Synthesis and Preliminary Biological Evaluation as Anti-Tumor Agents Fernandes, Sandra Meyer, Shea T. Shah, Jigisha P. Adhikari, Arijit A. Kerr, William G. Chisholm, John D. Molecules Article 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. MDPI 2022-12-02 /pmc/articles/PMC9738565/ /pubmed/36500543 http://dx.doi.org/10.3390/molecules27238451 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Fernandes, Sandra
Meyer, Shea T.
Shah, Jigisha P.
Adhikari, Arijit A.
Kerr, William G.
Chisholm, John D.
N1-Benzyl Tryptamine Pan-SHIP1/2 Inhibitors: Synthesis and Preliminary Biological Evaluation as Anti-Tumor Agents
title N1-Benzyl Tryptamine Pan-SHIP1/2 Inhibitors: Synthesis and Preliminary Biological Evaluation as Anti-Tumor Agents
title_full N1-Benzyl Tryptamine Pan-SHIP1/2 Inhibitors: Synthesis and Preliminary Biological Evaluation as Anti-Tumor Agents
title_fullStr N1-Benzyl Tryptamine Pan-SHIP1/2 Inhibitors: Synthesis and Preliminary Biological Evaluation as Anti-Tumor Agents
title_full_unstemmed N1-Benzyl Tryptamine Pan-SHIP1/2 Inhibitors: Synthesis and Preliminary Biological Evaluation as Anti-Tumor Agents
title_short N1-Benzyl Tryptamine Pan-SHIP1/2 Inhibitors: Synthesis and Preliminary Biological Evaluation as Anti-Tumor Agents
title_sort n1-benzyl tryptamine pan-ship1/2 inhibitors: synthesis and preliminary biological evaluation as anti-tumor agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9738565/
https://www.ncbi.nlm.nih.gov/pubmed/36500543
http://dx.doi.org/10.3390/molecules27238451
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