Journal article
Identification and preliminary structure-activity relationship studies of 1,5-dihydrobenzo[e][1,4]oxazepin-2(3H)-ones that induce differentiation of acute myeloid leukemia cells in vitro
- Abstract:
- Acute myeloid leukemia (AML) is the most aggressive type of blood cancer, and there is a continued need for new treatments that are well tolerated and improve long-term survival rates in patients. Induction of differentiation has emerged as a promising alternative to conventional cytotoxic chemotherapy, but known agents lack efficacy in genetically distinct patient populations. Previously, we established a phenotypic screen to identify small molecules that could stimulate differentiation in a range of AML cell lines. Utilising this strategy, a 1,5-dihydrobenzo[e][1,4]oxazepin-2(3H)-one hit compound was identified. Herein, we report the hit validation in vitro, structure-activity relationship (SAR) studies and the pharmacokinetic profiles for selected compounds.
- Publication status:
- Published
- Peer review status:
- Peer reviewed
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(Preview, Version of record, 7.9MB, Terms of use)
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- Publisher copy:
- 10.3390/molecules26216648
Authors
- Publisher:
- MDPI
- Journal:
- Molecules More from this journal
- Volume:
- 26
- Issue:
- 21
- Article number:
- 6648
- Publication date:
- 2021-11-02
- Acceptance date:
- 2021-10-18
- DOI:
- EISSN:
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1420-3049
- Pmid:
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34771052
- Language:
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English
- Keywords:
- Pubs id:
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1210481
- Local pid:
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pubs:1210481
- Deposit date:
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2021-12-07
Terms of use
- Copyright holder:
- Josa-Culleré et al.
- Copyright date:
- 2021
- Rights statement:
- Copyright © 2021 The Author(s). This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
- Licence:
- CC Attribution (CC BY)
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