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新的黄樟素衍生物及其对乳腺癌细胞的抗增殖活性。

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

机构信息

Departamento de Química, Universidad Técnica Federico Santa María, Av. España N° 1680, Valparaíso, Chile.

出版信息

Molecules. 2011 Jun 3;16(6):4632-41. doi: 10.3390/molecules16064632.

DOI:10.3390/molecules16064632
PMID:21642937
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6264777/
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 IC₅₀ 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).

摘要

从黄樟素合成儿茶酚。制备了 9 种衍生物,并使用不同的人细胞系评估其抗增殖作用。体外生长抑制试验基于磺基罗丹明染料来定量细胞活力。在对两种乳腺癌细胞系(MCF-7 和 MDA-MB-231)进行的测试中,化合物 4-烯丙基苯-1,2-二醇(3)、4-4-[3-(乙酰氧基)丙基]-1,2-苯二乙酸酯(6)和 4-[3-(乙酰氧基)丙基]-5-硝基-1,2-苯二乙酸酯(10)比母体化合物 2 显示出更高的细胞毒性。对于无皮肤人成纤维细胞(DHF 细胞)毒性,其 IC₅₀ 值分别为 40.2±6.9 μM、5.9±0.8 μM 和 33.8±4.9 μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2e22/6264777/31dd64be1fa5/molecules-16-04632-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2e22/6264777/31dd64be1fa5/molecules-16-04632-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2e22/6264777/31dd64be1fa5/molecules-16-04632-g001.jpg

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