title: Stephacidin A and B: two structurally novel, selective inhibitors of the testosterone-dependent prostate LNCaP cells.
abstract: Two novel antitumor alkaloids, Stephacidin A and B, were isolated from the solid fermentation of Aspergillus ochraceus WC76466. Both alkaloids exhibit in vitro cytotoxicity against a number of human tumor cell lines; however, stephacidin B demonstrated more potent and selective antitumor activities, especially against prostate testeosterone-dependent LNCaP cells with IC50 value of 60 nM. The structures of stephacidin A and B were established on the basis of the NMR data and X-ray crystallography. With 15 rings and 9 chiral centers, stephacidin B represents one of the most structurally complex and novel alkaloids occurring in nature.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA.
authors.forename: Jingfang
authors.initials: J
authors.lastname: Qian-Cutrone
authors.forename: Stella
authors.initials: S
authors.lastname: Huang
authors.forename: Yue-Zhong
authors.initials: YZ
authors.lastname: Shu
authors.forename: Dolatrai
authors.initials: D
authors.lastname: Vyas
authors.forename: Craig
authors.initials: C
authors.lastname: Fairchild
authors.forename: Ana
authors.initials: A
authors.lastname: Menendez
authors.forename: Kimberly
authors.initials: K
authors.lastname: Krampitz
authors.forename: Richard
authors.initials: R
authors.lastname: Dalterio
authors.forename: Steven E
authors.initials: SE
authors.lastname: Klohr
authors.forename: Qi
authors.initials: Q
authors.lastname: Gao
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D001235:Aspergillus ochraceus / Q000737:chemistry*; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D026121:Indole Alkaloids; D007211:Indoles / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D008297:Male; D015394:Molecular Structure; D009376:Neoplasms, Hormone-Dependent / Q000188:drug therapy* / Q000473:pathology; D019906:Nuclear Magnetic Resonance, Biomolecular; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013739:Testosterone / Q000502:physiology; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D026121:Indole Alkaloids; D007211:Indoles; C470895:stephacidin A; C470894:stephacidin B; D013739:Testosterone