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Synthesis and evaluation of a fluorescent ritterazine-cephalostatin hybrid.

ABSTRACT: 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.

SUBMITTER: Kumar KA

PROVIDER: S-EPMC3264888 | biostudies-literature | 2011 Oct

REPOSITORIES: biostudies-literature

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Synthesis and evaluation of a fluorescent ritterazine-cephalostatin hybrid.

Kumar Kanduluru Ananda KA La Clair James J JJ Fuchs Philip L PL

Organic letters 20110914 19

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 surr ...[more]

PMID: 21913733

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