Synthesis and Cytotoxic Activity of Some3-Benzyl-5-Arylidenefuran-2(5H)-ones

Molecules

R༻son Ricardo Teixeira²  Luiz Cláudio Almeida Barbosa²  Célia Regina Alvares Maltha²  Marcelo E๺ Rocha²  Daniel Pereira Bezerra¹  Letໜia Veras Costa-Lotufo¹  Cláudia Pessoa¹ 

[1] Department of Physiology and Pharmacology, Federal University of Ceará, Rua Coronel Nunes de Melo, 1127, CEP 60431-970, Fortaleza, CE, Brazil;Department of Chemistry, Federal University of Viçosa, Av. P.H. Rolfs, S/N, CEP 36570-000, Viçosa, MG, Brazil

关键词: Nostoclides;    cytotoxic activity;    lactones;    γ-alkylidenebutenolides;   

DOI  :  10.3390/12051101

来源: mdpi

【 摘 要 】

3-Benzyl-furan-2(5H)-one (2a) and 3-(4-bromobenzyl)-furan-2(5H)-one (2b) were treated with TBDMSOTf and converted into the corresponding tert-butyldimethyl-silylfuran ethers. These furans were further condensed with several aromatic aldehydes affording compounds 5-14 with general 3-benzyl-5-arylidene-furan-2(5H)-one structures in 31% to 98% yields. Such compounds are analogues of the naturally occurring nostoclide lactones, reported to present moderate cytotoxic activity. Compounds 5-14 were submitted to an in vitro bioassay against the HL-60, HCT-8, SF295 and MDA-MB-435 cancer cell lines using the MTT cytotoxicity assay.

【 授权许可】

Unknown   
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