Chemical modification of reveromycin A and its biological activities

Takeshi Shimizu; Takeo Usui; Kiyotaka Machida; Kouichi Furuya; Hiroyuki Osada; Tadashi Nakata

doi:10.1016/s0960-894x(02)00782-5

Chemical modification of reveromycin A and its biological activities

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3363-6. doi: 10.1016/s0960-894x(02)00782-5.

Authors

Takeshi Shimizu¹, Takeo Usui, Kiyotaka Machida, Kouichi Furuya, Hiroyuki Osada, Tadashi Nakata

Affiliation

¹ Synthetic Organic Chemistry Laboratory, RIKEN (The Institute of Physical and Chemical Research), Wako, Saitama, Japan. tshimizu@postman.riken.go.jp

PMID: 12419362
DOI: 10.1016/s0960-894x(02)00782-5

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Anti-Bacterial Agents / chemistry*
Anti-Bacterial Agents / pharmacology*
Cell Line, Transformed
Genes, src
Inhibitory Concentration 50
Isoleucine-tRNA Ligase / metabolism
Kidney / cytology
Kidney / metabolism
Pyrans / chemistry*
Pyrans / pharmacology*
Rats
Spiro Compounds / chemistry*
Spiro Compounds / pharmacology*
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Pyrans
Spiro Compounds
reveromycin A
Isoleucine-tRNA Ligase