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Synthesis and biology of 3 '-N-acyl-N-debenzoylpaclitaxel analogues

Authors
Roh, EJ; Song, CE; Kim, D; Pae, HO; Chung, HT; Lee, KS; Chai, KB; Lee, CO; Choi, SU
Issue Date
1999-09
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY, v.7, no.9, pp.2115 - 2119
Abstract
The 3'-N-acyl-N-debenzoylpaclitaxel analogues 1a-d were synthesized and evaluated on biological systems. Some of the analogues 1a-d exhibited higher cytotoxicities (up to 20-fold) and stronger abilities to induce apoptosis than paclitaxel. In an in vivo experiment against ip implanted B16 melanoma, the most cytotoxic compound 1b in vitro caused tumor growth inhibition more than paclitaxel. (C) 1999 Elsevier Science Ltd. All rights reserved.
Keywords
PROGRAMMED CELL-DEATH; TAXOL ANALOGS; APOPTOSIS; CYTOTOXICITY; MICROTUBULES; CISPLATIN; THERAPY; CANCER; LINES; PROGRAMMED CELL-DEATH; TAXOL ANALOGS; APOPTOSIS; CYTOTOXICITY; MICROTUBULES; CISPLATIN; THERAPY; CANCER; LINES; 3 ' -N-acyl-N-debenzoylpaclitaxel analogues; cytotoxicity; apoptosis; structure-activity relationship
ISSN
0968-0896
URI
https://pubs.kist.re.kr/handle/201004/141953
DOI
10.1016/S0968-0896(99)00173-X
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