Synthesis of yashabushidiol and its analogues and their cytotoxic activity against cancer cell lines.
Synthesis of yashabushidiol and its analogues and their cytotoxic activity against cancer cell lines.
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DOI：
10.1016/j.bmcl.2009.03.061
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发表时间：
2009-06
影响因子：
2.7
通讯作者：
M. Narasimhulu;T. S. Reddy;K. C. Mahesh;A. Sai Krishna;J. V. Rao;Y. Venkateswarlu
中科院分区：
文献类型：
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作者：
M. Narasimhulu;T. S. Reddy;K. C. Mahesh;A. Sai Krishna;J. V. Rao;Y. Venkateswarlu
通过用取代的苯乙炔对3-羟基-5-苯基戊醛进行炔基化，实现了yashabushidiol (1a)（一种具有1,3-二醇系统的直链二芳基庚烷及其类似物）的全合成。所有化合物均对人类白血病（THP-1、U-937）和黑色素瘤（A-375）细胞系显示出显着的抗增殖活性。发现化合物 2a 和 2b 对 THP-1 白血病细胞系最有效，IC50 分别为 12.82μg/mL 和 12.62μg/mL。
A total synthesis of yashabushidiol (1a), a linear diarylheptanoid having 1,3- diol system and its analogues has been achieved by alkynylation of 3-hydroxy-5-phenyl pentanal with substituted phenyl acetylenes. All the compounds have shown significant anti-proliferative activity on human leukemia (THP-1, U-937) and melanoma (A-375) cell lines. Compounds 2a and 2b were found to be most potent with an IC50of 12.82μg/mL and 12.62μg/mL, respectively, on THP-1 leukemia cell line.