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新型乳香酸衍生物的合成及其作为潜在的抗增殖剂。

Synthesis of new boswellic acid derivatives as potential antiproliferative agents.

机构信息

UoN Chair of Oman's Medicinal Plants and Marine Natural Products, University of Nizwa, Nizwa, Sultanate of Oman.

Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.

出版信息

Nat Prod Res. 2020 Jul;34(13):1845-1852. doi: 10.1080/14786419.2018.1564295. Epub 2019 Jan 29.

DOI:10.1080/14786419.2018.1564295
PMID:30691289
Abstract

In the current investigation, a series of heterocyclic derivatives of boswellic acids were prepared along with new monomers of 3--acetyl-11-keto-β-boswellic acid (AKBA, ) 11-keto-β-boswellic acid (KBA, ) and several new bis-AKBA and KBA homodimers and AKBA-KBA heterodimers. The effects of these compounds on the proliferation of different human cancer cell lines, viz., FaDu (pharynx carcinoma), A2780 (ovarian carcinoma), HT29 (colon adenocarcinoma), and A375 (malignant melanoma), have been evaluated. Thus, KBA homodimer effectively inhibited the growth of FaDu, A2780, HT29, and A375 cells with EC values below 9 μM. In addition, compounds , , , , , and also exhibited cytotoxic effects for A2780, HT29, and A375 cancer cells. In particular, the pyrazine analog was highly cytotoxic for A375 cancer cells with an EC value of 2.1 μM.

摘要

在当前的研究中,我们合成了一系列的乳香酸杂环衍生物以及新的单体化合物 3--乙酰基-11-酮-β-乳香酸(AKBA,)11-酮-β-乳香酸(KBA,),还有几个新的双 AKBA 和 KBA 同二聚体以及 AKBA-KBA 杂二聚体。我们评估了这些化合物对不同人类癌细胞系(例如 FaDu(咽癌)、A2780(卵巢癌)、HT29(结肠癌)和 A375(恶性黑色素瘤))增殖的影响。结果表明,KBA 同二聚体 能有效抑制 FaDu、A2780、HT29 和 A375 细胞的生长,其 EC 值低于 9 μM。此外,化合物 、、、、、和 对 A2780、HT29 和 A375 癌细胞也表现出细胞毒性作用。特别是吡嗪类似物 对 A375 癌细胞具有高细胞毒性,EC 值为 2.1 μM。

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