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KMID : 0043320140370101264
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Archives of Pharmacal Research
2014 Volume.37 No. 10 p.1264 ~ p.1270
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Asymmetric synthesis and evaluation of α-quaternary chiral lactam derivatives as novel anticancer agents
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Lee Hwan-Hyuk
Hwang Su-Jung
Jung Ji-Sung
Hong Suck-Chang
Lee Myung-Mo
Park Hyeung-Geun
Lee Hyo-Jong
Park Yo-Han
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Abstract
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Asymmetric synthesis of α-quaternary chiral lactam derivatives as novel anticancer agents and evaluation of their cytotoxic potentials and spectrums are reported. Among the developed lactam derivatives, the most active new compounds (S)-4m and (S)-4n synthesized via asymmetric phase-transfer catalytic alkylation in very high optical yields (98 % ee) show promising in vitro anticancer activities with low micromolar IC50 values against colon, uterus, lung, and breast human cancer cells.
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KEYWORD
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α-Quaternary chiral lactam, Phase-transfer catalytic alkylation, Colon, Lung, Breast cancers, Anticancer activity
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