4.4 Article

Synthesis and anticancer activity of novel halolactones with β-aryl substituents from simple aromatic aldehydes

期刊

TETRAHEDRON
卷 69, 期 48, 页码 10414-10423

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2013.09.094

关键词

Lactones; Aromatic ring; Halolactonization; Cytotoxic activity

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A series of 20 novel racemic iodo-, bromo- and chlorolactones, possessing beta-phenyl-gamma-lactone or beta-phenyl-delta-lactone framework, were synthesized from commercially available aromatic aldehydes in convenient five-step syntheses. Some of them showed noticeable cytotoxic effect against two cancer lines, Jurkat (human leukaemia) and D17 (canine osteosarcoma). The highest activity, comparable with carboplatin, was observed for cis-5-(1-iodoethyl)-4-(4'-isopropylphenyl)dihydrofuran-2-one against Jurkat cell line. (C) 2013 Elsevier Ltd. All rights reserved.

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