Journal
ORGANIC LETTERS
Volume 13, Issue 19, Pages 5334-5337Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol202139z
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Funding
- NIH [5U01CA060548-17, CA 60548]
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The cephalostatin and ritterazine natural products comprise a potent family of bis-steroidal pyrazines that display potent single-digit nanomolar inhibition of tumor cell growth. An active fluorescent ritterazine-cephalostatin hybrid probe was developed using detailed SAR data derived through total synthetic efforts. A combination of time course and confocal imaging studies indicate that this natural product family is rapidly taken up in tumor cells and localizes subcellularly within ER and surrounding the nuclear-ER interface.
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