Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.

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Title

Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.

Content partner

The University of Auckland Library

Collection

ResearchSpace@Auckland

Description

Replacing one of the morpholine groups of the phosphatidylinositol 3-kinase (PI3K) inhibitor ZSTK474 with a variety of sulfonamide-linked solubilizing substituents produced a new class of active and potent PI3Kα inhibitors, with several derivatives demonstrating high PI3Kα enzyme potency and good cellular potency in two human derived cell lines. The overall results suggest a preference for linear and somewhat flexible solubilizing functions. From this series, compound 16, also known as SN3297...

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Format

Research paper

Research format

Journal article

Date created

2019-4

Creator

Giddens, Anna C / Gamage, Swarna A / Kendall, Jackie D / Lee, Woo-Jeong / Baguley, Bruce C / Buchanan, Christina M / Jamieson, Stephen MF / Dickson, James MJ / Shepherd, Peter R / Denny, William A / Rewcastle, Gordon W

URL

https://hdl.handle.net/2292/58127

Related subjects

Cell Line, Tumor / Animals / Humans / Mice / Neoplasms / Sulfonamides / Triazines / Protein Subunits / Antineoplastic Agents / Transplantation, Heterologous / Drug Evaluation, Preclinical / Inhibitory Concentration 50 / Cell Proliferation / Structure-Activity Relationship / Female / Phosphatidylinositol 3-Kinases / Phosphoinositide-3 Kinase Inhibitors / PI3K / Phosphatidylinositol 3-kinase / SN32976 / ZSTK474 / p110α / Science & Technology / Life Sciences & Biomedicine / Physical Sciences / Biochemistry & Molecular Biology / Chemistry, Medicinal / Chemistry, Organic / Pharmacology & Pharmacy / Chemistry / p110 alpha / PHOSPHOINOSITIDE 3-KINASE / CLASS-I / PIK3CA GENE / ISOFORM / PATHWAY / KINASE / MECHANISMS / P110-ALPHA / DISCOVERY / 0601 Biochemistry and Cell Biology / 5.1 Pharmaceuticals / 0304 Medicinal and Biomolecular Chemistry / 0305 Organic Chemistry / 1115 Pharmacology and Pharmaceutical Sciences

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