Evaluation of antitumor properties of novel saframycin analogs in vitro and in vivo.
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.
Spencer
Jeffrey R
JR
Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA. jeffspencer.celera@mac.com
Sendzik
Martin
M
Oeh
Jason
J
Sabbatini
Peter
P
Dalrymple
Stacie A
SA
Magill
Catherine
C
Kim
Hyunjin M
HM
Zhang
Penglie
P
Squires
Neil
N
Moss
Katherine G
KG
Sukbuntherng
Juthamas
J
Graupe
Doris
D
Eksterowicz
John
J
Young
Peter R
PR
Myers
Andrew G
AG
Green
Michael J
MJ
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
D000970:Antineoplastic Agents; D007546:Isoquinolines; C026925:saframycin A