title: Evaluation of antitumor properties of novel saframycin analogs in vitro and in vivo.
abstract: Novel analogs of (-)-saframycin A are described. The analogs are shown to be potent inhibitors of the in vitro growth of several tumor cells in a broad panel and promising as leads for further optimization. The first in vivo studies in a solid tumor model (HCT-116) reveal potent antitumor activity with associated toxicity of daily administration.
authors.affiliation: Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA. jeffspencer.celera@mac.com
authors.forename: Jeffrey R
authors.initials: JR
authors.lastname: Spencer
authors.forename: Martin
authors.initials: M
authors.lastname: Sendzik
authors.forename: Jason
authors.initials: J
authors.lastname: Oeh
authors.forename: Peter
authors.initials: P
authors.lastname: Sabbatini
authors.forename: Stacie A
authors.initials: SA
authors.lastname: Dalrymple
authors.forename: Catherine
authors.initials: C
authors.lastname: Magill
authors.forename: Hyunjin M
authors.initials: HM
authors.lastname: Kim
authors.forename: Penglie
authors.initials: P
authors.lastname: Zhang
authors.forename: Neil
authors.initials: N
authors.lastname: Squires
authors.forename: Katherine G
authors.initials: KG
authors.lastname: Moss
authors.forename: Juthamas
authors.initials: J
authors.lastname: Sukbuntherng
authors.forename: Doris
authors.initials: D
authors.lastname: Graupe
authors.forename: John
authors.initials: J
authors.lastname: Eksterowicz
authors.forename: Peter R
authors.initials: PR
authors.lastname: Young
authors.forename: Andrew G
authors.initials: AG
authors.lastname: Myers
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Green
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051379:Mice; D008807:Mice, Inbred BALB C; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D007546:Isoquinolines; C026925:saframycin A