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设计、合成及新型 3-(噻吩-2-基硫代)吡啶衍生物的生物评价作为潜在的多靶点抗癌药物。

Design, synthesis, and biological evaluation of novel 3-(thiophen-2-ylthio)pyridine derivatives as potential multitarget anticancer agents.

机构信息

Department of Pharmaceutical Preparation, Hangzhou Xixi Hospital, Hangzhou, Zhejiang Province, China.

School of Medicine, Zhejiang University City College, Hangzhou, Zhejiang Province, China.

出版信息

Arch Pharm (Weinheim). 2019 Aug;352(8):e1900024. doi: 10.1002/ardp.201900024. Epub 2019 Jul 24.

DOI:10.1002/ardp.201900024
PMID:31338897
Abstract

A series of novel 3-(thiophen-2-ylthio)pyridine derivatives as insulin-like growth factor 1 receptor (IGF-1R) inhibitors was designed and synthesized. IGF-1R kinase inhibitory activities and cytotoxicities against HepG2 and WSU-DLCL2 cell lines were tested. For all of these compounds, potent cancer cell proliferation inhibitory activities were observed, but not through the inhibition of IGR-1R. Selected compounds were further screened against various kinases. Typical compound 22 (50% inhibitory concentration [IC ] values, HepG2: 2.98 ± 1.11 μM and WSU-DLCL2: 4.34 ± 0.84 μM) exhibited good inhibitory activities against fibroblast growth factor receptor-2 (FGFR2), FGFR3, epidermal growth factor receptor, Janus kinase, and RON (receptor originated from Nantes), with IC values ranging from 2.14 to 12.20 μM. Additionally, the cell-cycle analysis showed that compound 22 could arrest HepG2 cells in the G1/G0 phase. Taken together, all the experiments confirmed that the compounds in this series were multitarget anticancer agents worth further optimizing.

摘要

设计并合成了一系列新型 3-(噻吩-2-基硫代)吡啶衍生物作为胰岛素样生长因子 1 受体 (IGF-1R) 抑制剂。测试了这些化合物对 HepG2 和 WSU-DLCL2 细胞系的 IGF-1R 激酶抑制活性和细胞毒性。对于所有这些化合物，都观察到了很强的癌细胞增殖抑制活性，但不是通过抑制 IGF-1R 实现的。选择的化合物进一步针对各种激酶进行了筛选。典型的化合物 22（对 HepG2 的 50%抑制浓度 [IC ] 值为 2.98 ± 1.11 μM，对 WSU-DLCL2 的为 4.34 ± 0.84 μM）对成纤维细胞生长因子受体 2 (FGFR2)、FGFR3、表皮生长因子受体、Janus 激酶和 RON（源自 Nantes 的受体）表现出良好的抑制活性，IC 值范围为 2.14 至 12.20 μM。此外，细胞周期分析表明，化合物 22 可以使 HepG2 细胞停滞在 G1/G0 期。总之，所有实验都证实，该系列化合物是值得进一步优化的多靶抗癌药物。

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