New catechol derivatives of safrole and their antiproliferative activity towards breast cancer cells

黄樟素的新型儿茶酚衍生物及其对乳腺癌细胞的抗增殖活性

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作者:Alejandro Madrid Villegas, Luis Espinoza Catalán, Iván Montenegro Venegas, Joan Villena García, Héctor Carrasco Altamirano

Abstract

Catechols were synthesized from safrole. Nine derivatives were prepared and assessed for antiproliferative effects using different human cell lines. The in vitro growth inhibition assay was based on the sulphorhodamine dye to quantify cell viability. The derivatives 4-allylbenzene-1,2-diol (3), 4 4-[3-(acetyloxy)propyl]-1,2-phenylene diacetate (6) and 4-[3-(acetyloxy)propyl]-5-nitro-1,2-phenylene diacetate (10) showed higher cytotoxicity than the parent compound 2 in tests performed on two breast cancer cell lines (MCF-7 and MDA-MB-231). The IC₅&sub0; values of 40.2 ± 6.9 μM, 5.9 ± 0.8 μM and 33.8 ± 4.9 μM, respectively, were obtained without toxicity towards dermal human fibroblast (DHF cells).

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