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Stephacidin A and B: two structurally novel, selective inhibitors of the testosterone-dependent prostate LNCaP cells.
Qian-Cutrone, Jingfang; Huang, Stella; Shu, Yue-Zhong; Vyas, Dolatrai; Fairchild, Craig; Menendez, Ana; Krampitz, Kimberly; Dalterio, Richard; Klohr, Steven E; Gao, Qi.
Afiliação
  • Qian-Cutrone J; Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA.
J Am Chem Soc ; 124(49): 14556-7, 2002 Dec 11.
Article em En | MEDLINE | ID: mdl-12465964
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.
Assuntos
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Base de dados: MEDLINE Assunto principal: Neoplasias da Próstata / Aspergillus ochraceus / Indóis / Neoplasias Hormônio-Dependentes / Antineoplásicos Idioma: En Ano de publicação: 2002 Tipo de documento: Article
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Base de dados: MEDLINE Assunto principal: Neoplasias da Próstata / Aspergillus ochraceus / Indóis / Neoplasias Hormônio-Dependentes / Antineoplásicos Idioma: En Ano de publicação: 2002 Tipo de documento: Article