期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 5, 期 6, 页码 662-667出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml500030p
关键词
BCL-X-L; BCL-2; apoptosis; cancer
资金
- Australian Research Council
- National Health and Medical Research Council (NHMRC) [305536, 257502, 461221, 1016701]
- Leukemia and Lymphoma Society [7015, 7413]
- Cancer Council of Victoria [461239]
- Australian Cancer Research Foundation
- NHMRC Independent Research Institutes Infrastructure Support Scheme [361646]
Because of the promise of BCL-2 antagonists in combating chronic lymphocytic leukemia (CLL) and non-Hodgkin's lymphoma (NHL), interest in additional selective antagonists of antiapoptotic proteins has grown. Beginning with a series of selective, potent BCL-X-L antagonists containing an undesirable hydrazone functionality, in silico design and X-ray crystallography were utilized to develop alternative scaffolds that retained the selectivity and potency of the starting compounds.
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