Discovery of a fluoroindolo[2,3-a]carbazole clinical candidate with broad spectrum antitumor activity in preclinical tumor models superior to the marketed oncology drug, CPT-11

Journal of Medicinal Chemistry

Volumn 48, Issue 7, 2005, Pages 2258-2261

  Saulnier, Mark G ^a   Balasubramanian, Balu N ^a   Long, Byron H ^a   Frennesson, David B ^a   Ruediger, Edward ^a   Zimmermann, Kurt ^a   Eummer, Jeffrey T ^a   St Laurent, Denis R ^a   Stoffan, Karen M ^a   Naidu, B Narasimhulu ^a   Mahler, Mikael ^a   Beaulieu, Francis ^a   Bachand, Carol ^a   Lee, Frank Y ^a   Fairchild, Craig R ^a   Stadnick, Linda K ^a   Rose, William C ^a   Solomon, Carola ^a   Wong, Henry ^a   Martel, Alain ^a   Wright, John J ^a   Kramer, Robert ^a   Langley, David R ^a   Vyas, Dolatrai M ^a   more..

^a NONE

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; BMS 250749; CAMPTOTHECIN; CARBAZOLE DERIVATIVE; DNA TOPOISOMERASE; FLUOROINDOLO[2,3 A]CARBAZOLE; IRINOTECAN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CONTROLLED STUDY; CYTOTOXICITY; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG STRUCTURE; ENZYME ACTIVITY; GLYCOSYLATION; HUMAN; LEWIS CARCINOMA; NONHUMAN;

ANIMALS; ANTINEOPLASTIC AGENTS; CAMPTOTHECIN; CARBAZOLES; CELL LINE, TUMOR; DNA TOPOISOMERASES, TYPE I; DRUG EVALUATION, PRECLINICAL; DRUG RESISTANCE, NEOPLASM; DRUG SCREENING ASSAYS, ANTITUMOR; GLUCOSIDES; HUMANS; INDOLES; MICE; MICROSOMES, LIVER; TRANSPLANTATION, HETEROLOGOUS;

EID: 20244372565     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm049090z     Document Type: Article

References (27)

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27. 50 = 1500 nM). Poor cell permeability of this 2′-fluoro analogue may account for its weak cytotoxicity.