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Identification and Preliminary Structure-Activity Relationship Studies of 1,5-Dihydrobenzo[ e ][1,4]oxazepin-2(3 H)-ones That Induce Differentiation of Acute Myeloid Leukemia Cells In Vitro.
- Source :
-
Molecules . Nov2021, Vol. 26 Issue 21, p6648. 1p. - Publication Year :
- 2021
-
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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 14203049
- Volume :
- 26
- Issue :
- 21
- Database :
- Academic Search Index
- Journal :
- Molecules
- Publication Type :
- Academic Journal
- Accession number :
- 153603096
- Full Text :
- https://doi.org/10.3390/molecules26216648