Total synthesis as a resource in the discovery of potentially valuable antitumor agents: Cycloproparadicicol Journal Article
| Authors: | Yamamoto, K.; Garbaccio, R. M.; Stachel, S. J.; Solit, D. B.; Chiosis, G.; Rosen, N.; Danishefsky, S. J. |
| Article Title: | Total synthesis as a resource in the discovery of potentially valuable antitumor agents: Cycloproparadicicol |
| Abstract: | A highly convergent synthesis was used to prepare a series of epimers and analogues of radicicol (1). Biological assessment revealed a previously unrecognized correlation between stereochemistry and antitumor potential in these compounds. Significantly, cycloproparadicicol (2) showed promising therapeutic properties based on inhibition of chaperones. |
| Keywords: | controlled study; unclassified drug; human cell; antineoplastic agents; antineoplastic agent; binding affinity; protein function; cell division; cell growth; protein binding; antineoplastic activity; cytotoxicity; drug structure; tumor cells, cultured; drug design; drug synthesis; structure activity relation; structure-activity relationship; breast neoplasms; cancer inhibition; cyclopropanes; tumors; heat shock protein 90; hsp90 heat-shock proteins; molecular structure; drug therapy; inhibitory concentration 50; cell strain mcf 7; cell cycle g1 phase; reaction analysis; drug protein binding; chemical reaction; synthesis (chemical); antitumor agents; structure-activity relationships; binding competition; stereochemistry; protein synthesis inhibition; growth inhibition; radicicol; cycloproparadicicol; lactones; natural products; cyclopropanation; macrolides; organic compounds; binding assay; humans; human; article; chaperone proteins; synthesis design |
| Journal Title: | Angewandte Chemie - International Edition |
| Volume: | 42 |
| Issue: | 11 |
| ISSN: | 1433-7851 |
| Publisher: | Wiley Blackwell |
| Date Published: | 2003-03-17 |
| Start Page: | 1280 |
| End Page: | 1284 |
| Language: | English |
| DOI: | 10.1002/anie.200390329 |
| PUBMED: | 12645064 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Export Date: 12 September 2014 -- Source: Scopus |
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