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取代戊酸的合成、抗癌活性、构效关系及相互作用结合模式研究。

Synthesis, anticancer activity, structure-activity relationship and binding mode of interaction studies of substituted pentanoic acids.

机构信息

Natural Science Laboratory, Division of Medicinal & Pharmaceutical Chemistry, Department of Pharmaceutical Technology, Jadavpur University, PO Box 17020, Kolkata 700032, West Bengal, India.

Department of Chemical Technology, University of Calcutta, 92 APC Ray Road, Kolkata 700009, India.

出版信息

Future Med Chem. 2019 Jul;11(14):1679-1702. doi: 10.4155/fmc-2018-0361. Epub 2019 Aug 2.

Abstract

Simultaneous inhibition of MMP-2 and HDAC8 may be an effective strategy to target cancer. In continuation of our earlier efforts, a series of substituted pentanoic acids (-) were synthesized and checked for their biological activity along with some earlier reported compounds (). Compounds and were found to induce apoptosis effectively in a dose-dependent fashion in Jurkat-E6.1 cell line. They reduced the expression of both MMP-2 and HDAC8 effectively. also produced prominent intensity of fluorescence to bring nick in Jurkat-E6.1 cells. also showed cellular arrest in sub-G0 phase. Such compounds may be useful to battle against cancer.

摘要

同时抑制 MMP-2 和 HDAC8 可能是针对癌症的有效策略。继我们早期的努力之后,我们合成了一系列取代的戊酸(-),并与一些早期报道的化合物()一起检查了它们的生物活性。在 Jurkat-E6.1 细胞系中,化合物和以剂量依赖性方式有效地诱导细胞凋亡。它们有效地降低了 MMP-2 和 HDAC8 的表达。还产生了明显的荧光强度,使 Jurkat-E6.1 细胞发生缺口。也显示出细胞在亚 G0 期的停滞。这些化合物可能有助于对抗癌症。

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