Chemical modification of reveromycin A and its biological activities.
Various derivatives of reveromycin A, a novel inhibitor of eukaryotic cell growth, were prepared and their inhibitory effects on both isoleucyl-tRNA synthetase activity and in vitro protein synthesis, and activities on the morphological reversion of src(ts)-NRK cells were assayed. The C5 hydroxyl group and C24 carboxyl group are particularly important for these activities.
Shimizu
Takeshi
T
Synthetic Organic Chemistry Laboratory, RIKEN (The Institute of Physical and Chemical Research), Wako, Saitama, Japan. tshimizu@postman.riken.go.jp
Usui
Takeo
T
Machida
Kiyotaka
K
Furuya
Kouichi
K
Osada
Hiroyuki
H
Nakata
Tadashi
T
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D002461:Cell Line, Transformed; D016391:Genes, src; D020128:Inhibitory Concentration 50; D007533:Isoleucine-tRNA Ligase / Q000378:metabolism; D007668:Kidney / Q000166:cytology / Q000378:metabolism; D011714:Pyrans / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D013141:Spiro Compounds / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D011714:Pyrans; D013141:Spiro Compounds; C068098:reveromycin A; D007533:Isoleucine-tRNA Ligase