- Abstract:
-
Recent literature has both suggested and questioned MTH1 as a novel cancer target. BAY-707 was just published as a target validation small molecule probe for assessing the effects of pharmacological inhibition of MTH1 on tumor cell survival, both in vitro and in vivo. (1) In this report, we describe the medicinal chemistry program creating BAY-707, where fragment-based methods were used to develop a series of highly potent and selective MTH1 inhibitors. Using structure-based drug design and r...
Expand abstract - Publication status:
- Published
- Peer review status:
- Peer reviewed
- Version:
- Accepted Manuscript
- Files:
-
-
(pdf, 1.3MB)
-
- Publisher copy:
- 10.1021/acs.jmedchem.7b01884
-
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- Publisher:
- American Chemical Society Publisher's website
- Journal:
- Journal of Medicinal Chemistry Journal website
- Volume:
- 61
- Issue:
- 6
- Pages:
- 2533–2551
- Publication date:
- 2018-02-27
- DOI:
- EISSN:
-
1520-4804
- ISSN:
-
0022-2623
- Pubs id:
-
pubs:828329
- URN:
-
uri:669bb577-bb66-4555-938c-49a866081107
- UUID:
-
uuid:669bb577-bb66-4555-938c-49a866081107
- Local pid:
- pubs:828329
- Language:
- English
- Copyright holder:
- American Chemical Society
- Copyright date:
- 2018
- Notes:
-
Copyright © 2018 American Chemical Society. This is the accepted manuscript version of the article. The final version is available online from American Chemical Society at: https://doi.org/10.1021/acs.jmedchem.7b01884
Journal article
Creation of a novel class of potent and selective MutT Homologue 1 (MTH1) inhibitors using fragment-based screening and structure-based drug design
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