2000年
Synthesis and tumor-promoting activities of 12-Epi-phorbol-12,13-dibutyrate
Bioscience, Biotechnology and Biochemistry
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- 巻
- 64
- 号
- 11
- 開始ページ
- 2429
- 終了ページ
- 2436
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1271/bbb.64.2429
12-Epi-phorbol-12,13-dibutyrate (1), the C12-epimer of the most frequently used phorbol ester probe, phorbol-12,13-dibutyrate (PDBu), has been synthesized from phorbol in 9 steps in order to investigate the structural requirements for tumor-promoting activity. Compound 1 showed about 100-fold weaker in vitro biological activities related to in vivo tumor promotion, Epstein-Barr virus early antigen (EBV-EA)-inducing ability, superoxide (O2 −) generation-inducing ability, and binding to the protein kinase C (PKC) regulatory domain surrogate peptides. The results indicated that the β-stereochemistry at position 12 of the phorbol skeleton is important for optimal activity. Binding selectivity to each PKC C1 domain of 1 was almost equal to that of PDBu. © 2000, Taylor &
Francis Group, LLC. All rights reserved.
Francis Group, LLC. All rights reserved.
- リンク情報
- ID情報
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- DOI : 10.1271/bbb.64.2429
- ISSN : 1347-6947
- ISSN : 0916-8451
- PubMed ID : 11193412
- SCOPUS ID : 0034330917