期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 19, 页码 6220-6224出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm8006195
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资金
- NCI Cancer Center [CA21765]
- American Lebanese Syrian Associated Charities (ALSAC)
- St. Jude Children's Research Hospital
We report the design and highly enantioselective synthesis of a potent analogue of the spliceosome inhibitor FR901464, based on a non-natural product scaffold. The design of this compound was facilitated by a pharmacophore hypothesis that assumed key interaction types that are common to FR901464 and an otherwise unrelated natural product (pladienolide). The synthesis allows for the preparation of numerous novel analogues. We present results on the in vitro activity for this compound against several tumor cell lines.
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