期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 11, 页码 2941-2959出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.03.079
关键词
Xanthones; Xanthen-9-ones; Antitumor; Benzopyran; Chromans; Chromene; Lipophilicity; Solubility
资金
- FCT-Fundacao para a Ciencia e Tecnologia [CEQUIMED-PESt.OE/SAU/UI4040/2011]
- FEDER funds through the COMPETE program [FCOMP-01-0124-FEDER-011057]
- FCT [PTDC/SAU-FCT/100930/2008, SFRH/BD/41165/2007, SRH/BPD/68787/2010]
- Santander Totta
- FAPESP (Brazil)
- CAPES (Brazil)
- Fundação para a Ciência e a Tecnologia [SFRH/BD/41165/2007] Funding Source: FCT
A promising antitumor xanthone derivative was optimized following a multidimensional approach that involved the synthesis of 17 analogues, the study of their lipophilicity and solubility, and the evaluation of their growth inhibitory activity on four human tumor cell lines. A new synthetic route for the hit xanthone derivative was also developed and applied for the synthesis of its analogues. Among the used cell lines, the HL-60 showed to be in general more sensitive to the compounds tested, with the most potent compound having a GI(50) of 5.1 mu M, lower than the hit compound. Lipophilicity was evaluated by the partition coefficient (K-p) of a solute between buffer and two membrane models, namely liposomes and micelles. The compounds showed a log K-p between 3 and 5 and the two membrane models showed a good correlation (r(2) = 0.916) between each other. Studies concerning relationship between solubility and structure were developed for the hit compound and 5 of its analogues. (C) 2013 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据