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KMID : 0043320130360070812
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Archives of Pharmacal Research
2013 Volume.36 No. 7 p.812 ~ p.831
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Design, synthesis, in vitro cytotoxicity evaluation and structure?activity relationship of Goniothalamin analogs
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Mohideen Mazlin
Zulkepli Suraya
Nik Salleh Nik Salmah
Zulkefeli Mohd
Weber Jean Frederic Faizal Abdullah
Rahman A. F. M. Motiur
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Abstract
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A series of six/five member (E/Z)-Goniothalamin analogs were synthesized from commercially available (3,4-dihydro-2H-pyran-2-yl)methanol/5-(hydroxymethyl)dihydrofuran-2(3H)-one in three steps with good to moderate overall yields and their cytotoxicity against lymphoblastic leukemic T cell line (Jurkat E6.1) have been evaluated. Among the synthesized analogs, (Z)-Goniothalamin appeared to be the most active in cytotoxicity (IC50 = 12 μM). Structure?activity relationship study indicates that introducing substituent in phenyl ring or replacing phenyl ring by pyridine/naphthalene, or decreasing the ring size of lactones (from six to five member) do not increase the cytotoxicity.
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KEYWORD
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E-Goniothalamin, Z-Goniothalamin, Cytotoxicity, Jurkat E6.1
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