Design and total synthesis of a superior family of epothilone analogues, which eliminate xenograft tumors to a nonrelapsable state Journal Article
| Authors: | Chou, T. C.; Dong, H.; Rivkin, A.; Yoshimura, F.; Gabarda, A. E.; Cho, Y. S.; Tong, W. P.; Danishefsky, S. J. |
| Article Title: | Design and total synthesis of a superior family of epothilone analogues, which eliminate xenograft tumors to a nonrelapsable state |
| Abstract: | Unusually promising profiles of antitumor activity are displayed by 26-trifluoro-(E)-9,10-dehydro-dEpoB (1), the design and practical total synthesis of which is described. This compound promotes tumor shrinkage and disappearance in human xenografts in nude mice at well-tolerated doses, with complete remission for over two months and early rapid recovery of body weight to the pretreatment control levels. |
| Keywords: | unclassified drug; drug tolerability; dose response; nonhuman; antineoplastic agents; paclitaxel; antineoplastic agent; neoplasm; neoplasms; mouse; animal; metabolism; animals; mice; body weight; relapse; drug screening; drug screening assays, antitumor; tumor cells, cultured; drug synthesis; structure activity relation; structure-activity relationship; docetaxel; cancer inhibition; xenograft; cell culture; nude mouse; mice, nude; tumors; remission; microtubule assembly; neoplasm transplantation; tumor growth; convalescence; models, chemical; synthesis; synthesis (chemical); antitumor agents; structure-activity relationships; epothilones; epothilone b; epothilone derivative; growth inhibition; cancer transplantation; natural products; chemical model; organic compounds; drug dosage; conformation analysis; humans; human; article; tumor shrinkage; 12,13 desoxyepothilone; 26 trifluoro 9,10 dehydroepothilone b; 9,10 dehydro 26 trifluoroepothilone derivative |
| Journal Title: | Angewandte Chemie - International Edition |
| Volume: | 42 |
| Issue: | 39 |
| ISSN: | 1433-7851 |
| Publisher: | Wiley Blackwell |
| Date Published: | 2003-10-13 |
| Start Page: | 4762 |
| End Page: | 4767 |
| Language: | English |
| PUBMED: | 14562342 |
| PROVIDER: | scopus |
| DOI: | 10.1002/anie.200352361 |
| DOI/URL: | |
| Notes: | Export Date: 12 September 2014 -- Source: Scopus |
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