Synthesis, chiral resolution, and determination of novel furan lignan derivatives with potent anti-tumor activity

Two chiral furan lignan was synthesized, chiral separated and their absolute configuration was determined by circular dichroism spectra. Compound 2c (IC 50 = 12 μM on QGY-7701), the racemate of 2a and 2b, is reported. A kind of racemic furan lignans were synthesized via a novel route, and two optica...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (6), p.1961-1964
Hauptverfasser: Sun, Hai Ling, Wang, Tian Tian, Lv, Zhi Liang, Feng, Ji Lu, Geng, Dong Ping, Li, Yong Mei, Li, Ke
Format: Artikel
Sprache:eng
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Zusammenfassung:Two chiral furan lignan was synthesized, chiral separated and their absolute configuration was determined by circular dichroism spectra. Compound 2c (IC 50 = 12 μM on QGY-7701), the racemate of 2a and 2b, is reported. A kind of racemic furan lignans were synthesized via a novel route, and two optical isomers were obtained through a selective hydrolization. The absolute configurations were determined by circular dichroism spectroscopy after separated through a preparative column. The different activities of isomers and the racemates were evaluated on QGY-7701 and HeLa cell lines, and compound 2c showed the best activity on QGY-7701 and HeLa cell lines with IC 50 12 μM and 13 μM, respectively.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.01.122