Synthesis and preliminary assessment of the anticancer and Wnt/β-catenin inhibitory activity of small amide libraries of fenamates and profens

Bini Mathew; Judith V. Hobrath; Wenyan Lu; Yonghe Li; Robert C. Reynolds

doi:10.1007/s00044-017-2001-z

Synthesis and preliminary assessment of the anticancer and Wnt/β-catenin inhibitory activity of small amide libraries of fenamates and profens

Bini Mathew
, Judith V. Hobrath
, Wenyan Lu
, Yonghe Li
, Robert C. Reynolds (Lead / Corresponding author)

Research output: Contribution to journal › Article › peer-review

20 Citations (Scopus)

243 Downloads (Pure)

Abstract

As part of an ongoing program to study the anticancer activity of non-steroidal anti-inflammatory drugs (NSAIDs) through generating diversity libraries of multiple NSAID scaffolds, we synthesized a series of NSAID amide derivatives and screened these sets against three cancer cell lines (prostate, colon and breast) and Wnt/β-catenin signaling. The evaluated amide analog libraries show significant anticancer activity/cell proliferation inhibition, and specific members of the sets show inhibition of Wnt/β-catenin signaling.

Original language	English
Pages (from-to)	3038-3045
Number of pages	8
Journal	Medicinal Chemistry Research
Volume	26
Issue number	11
Early online date	5 Aug 2017
DOIs	https://doi.org/10.1007/s00044-017-2001-z
Publication status	Published - Nov 2017

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Amides
Cancer
Fenamates
NSAIDs
Wnt/β-catenin

ASJC Scopus subject areas

Pharmacology, Toxicology and Pharmaceutics(all)
Organic Chemistry

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10.1007/s00044-017-2001-zLicence: CC BY

Final Published Version
Open Access This article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://crea tivecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made
Final published version, 673 KBLicence: CC BY

Cite this

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title = "Synthesis and preliminary assessment of the anticancer and Wnt/β-catenin inhibitory activity of small amide libraries of fenamates and profens",

abstract = "As part of an ongoing program to study the anticancer activity of non-steroidal anti-inflammatory drugs (NSAIDs) through generating diversity libraries of multiple NSAID scaffolds, we synthesized a series of NSAID amide derivatives and screened these sets against three cancer cell lines (prostate, colon and breast) and Wnt/β-catenin signaling. The evaluated amide analog libraries show significant anticancer activity/cell proliferation inhibition, and specific members of the sets show inhibition of Wnt/β-catenin signaling.",

keywords = "Amides, Cancer, Fenamates, NSAIDs, Wnt/β-catenin",

author = "Bini Mathew and Hobrath, \{Judith V.\} and Wenyan Lu and Yonghe Li and Reynolds, \{Robert C.\}",

note = "This work was supported by grants from the National Institutes of Health NCI 1R01CA131378 (RCR PI) and RO1CA124531 (Y. Li PI). We also acknowledge DOD Era of Hope award W81XWH-07-1-0463 (RCR PI) for supporting HTS cancer cell activity profiling.",

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month = nov,

doi = "10.1007/s00044-017-2001-z",

language = "English",

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T1 - Synthesis and preliminary assessment of the anticancer and Wnt/β-catenin inhibitory activity of small amide libraries of fenamates and profens

AU - Mathew, Bini

AU - Hobrath, Judith V.

AU - Lu, Wenyan

AU - Li, Yonghe

AU - Reynolds, Robert C.

N1 - This work was supported by grants from the National Institutes of Health NCI 1R01CA131378 (RCR PI) and RO1CA124531 (Y. Li PI). We also acknowledge DOD Era of Hope award W81XWH-07-1-0463 (RCR PI) for supporting HTS cancer cell activity profiling.

PY - 2017/11

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N2 - As part of an ongoing program to study the anticancer activity of non-steroidal anti-inflammatory drugs (NSAIDs) through generating diversity libraries of multiple NSAID scaffolds, we synthesized a series of NSAID amide derivatives and screened these sets against three cancer cell lines (prostate, colon and breast) and Wnt/β-catenin signaling. The evaluated amide analog libraries show significant anticancer activity/cell proliferation inhibition, and specific members of the sets show inhibition of Wnt/β-catenin signaling.

AB - As part of an ongoing program to study the anticancer activity of non-steroidal anti-inflammatory drugs (NSAIDs) through generating diversity libraries of multiple NSAID scaffolds, we synthesized a series of NSAID amide derivatives and screened these sets against three cancer cell lines (prostate, colon and breast) and Wnt/β-catenin signaling. The evaluated amide analog libraries show significant anticancer activity/cell proliferation inhibition, and specific members of the sets show inhibition of Wnt/β-catenin signaling.

KW - Amides

KW - Cancer

KW - Fenamates

KW - NSAIDs

KW - Wnt/β-catenin

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U2 - 10.1007/s00044-017-2001-z

DO - 10.1007/s00044-017-2001-z

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AN - SCOPUS:85026816221

SN - 1054-2523

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SP - 3038

EP - 3045

JO - Medicinal Chemistry Research

JF - Medicinal Chemistry Research

IS - 11

ER -

Synthesis and preliminary assessment of the anticancer and Wnt/β-catenin inhibitory activity of small amide libraries of fenamates and profens

Abstract

UN SDGs

Keywords

ASJC Scopus subject areas

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