Preparation of amino acid conjugates of betulinic acid with activity against human melanoma

Preparation of amino acid conjugates of betulinic acid with activity against human melanoma
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DOI:
10.1016/s0960-894x(99)00165-1
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发表时间:
1999-04-19
影响因子:
2.7
通讯作者:
Kim, DSHL
Kim, DSHL
中科院分区:
医学4区
文献类型:
--
作者:
Jeong, HJ;Chai, HB;Kim, DSHL

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白桦酸在C-28位与一系列氨基酸偶联,对培养的人黑色素瘤(MEL-2)和口腔表皮样癌(KB)细胞株的毒性进行了评价。白桦酸的一些氨基酸结合物表现出更好的水溶性和选择性的细胞毒性。这项研究表明,白桦酸的氨基酸结合物可以产生潜在的重要衍生物,这些衍生物可能被开发为抗肿瘤药物。(C)1999爱思唯尔科学有限公司。保留所有权利。
Betulinic acid has been coupled with a series of amino acids at C-28 carboxylic acid position and the toxicity of the derivatives has been evaluated against cultured human melanoma (MEL-2) and human epidermoid carcinoma of the mouth (KB) cell lines. A number of amino acid conjugates of betulinic acid showed improved water solubility as well as selective cytotoxicity. This investigation demonstrates that amino acid conjugates of betulinic acid can produce potentially important derivatives, which may be developed as antitumor agents. (C) 1999 Elsevier Science Ltd. All rights reserved.