title: 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.
authors.affiliation: Department of Chemistry, Purdue University, West Lafayette, Indiana 47907, USA.
authors.forename: Kanduluru Ananda
authors.initials: KA
authors.lastname: Kumar
authors.forename: James J
authors.initials: JJ
authors.lastname: La Clair
authors.forename: Philip L
authors.initials: PL
authors.lastname: Fuchs
mesh_terms: D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000378:metabolism; D045325:HCT116 Cells; D006801:Humans; D015394:Molecular Structure; D010619:Phenazines / Q000138:chemical synthesis* / Q000378:metabolism; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000378:metabolism; D013256:Steroids / Q000138:chemical synthesis* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D005456:Fluorescent Dyes; D010619:Phenazines; D013141:Spiro Compounds; D013256:Steroids