Preparation of betulinic acid derivatives by chemical and biotransformation methods and determination of cytotoxicity against selected cancer cell lines
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- 作者：Leopoldo C. Baratto ; Mariana V. Porsani ; Ida C. Pimentel ; Adaucto B. Pereira Netto ; Reinhard Paschke ; Br¨¢s H. Oliveira
- 关键词：Betulinic acid ; Antitumor activity ; Cytotoxicity ; Biotransformation ; SRB assay
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2013
- 出版时间：October, 2013
- 年：2013
- 卷：68
- 期：Complete
- 页码：121-131
- 全文大小：1380 K
文摘
Several novel 2,4-dinitrophenylhydrazone betulinic acid derivatives have been prepared by chemical and biotransformation methods using fungi and carrot cells. Some compounds showed significant cytotoxicity and selectivity against some tumor cell lines. The most active, 3-[(2,4-dinitrophenyl)hydrazono]lup-(20R)-29-oxolupan-28-oic acid, showed IC50 values between 1.76 and 2.51?¦ÌM against five human cancer cell lines. The most selective, 3-hydroxy-20-[(2,4-dinitrophenyl)hydrazono]-29-norlupan-28-oic acid, was five to seven times more selective for cancer cells when compared to fibroblasts. Cell cycle analysis and apoptosis induction were studied for the most active derivatives.