Highly selective anti-cancer agents targeting non-small cell lung cancer and other forms of cancer

Described herein are analogs of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogs having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed.
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Abstract/Description: Described herein are analogs of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogs having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed.
Subject(s): C07D277/22
C07D277/24
Date Issued: 2019-08-27
Title: Highly selective anti-cancer agents targeting non-small cell lung cancer and other forms of cancer.
Name(s): Tillekeratne, Viranga, inventor
Taylor, William, inventor
Fedorka, Sara, inventor
The University of Toledo, assignee
Type of Resource: text
Genre: patent
Date Issued: 2019-08-27
Other Date: Date Filed: 2018-09-25
Publisher: United States Patent and Trademark Office
Physical Form: application/pdf
Extent: 18 p.
Abstract/Description: Described herein are analogs of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogs having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed.
Identifier(s): utpatents-US10392354 (IID)
Patent No.: US10392354 (patno)
Appl. No.: 16/141595 (appno)
Subject(s): C07D277/22
C07D277/24
Held by: United States Patent and Trademark Office (USPTO) Public Search Facility
Location: University of Toledo Digital Repository
Rights Statement: No Copyright - United States
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