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肉桂酸和迷迭香碱的新型硫化衍生物作为信号转导与转录激活因子3（STAT3）和核因子κB（NF-κB）转录因子的抑制剂

New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB transcription factors.

作者信息

Gabriele Elena, Brambilla Dario, Ricci Chiara, Regazzoni Luca, Taguchi Kyoko, Ferri Nicola, Asai Akira, Sparatore Anna

机构信息

a Department of Pharmaceutical Sciences , Università degli Studi di Milano , Milano , Italy.

b Department of Pharmacological and Biomolecular Sciences , Università degli Studi di Milano , Milano , Italy.

出版信息

J Enzyme Inhib Med Chem. 2017 Dec;32(1):1012-1028. doi: 10.1080/14756366.2017.1350658.

DOI:10.1080/14756366.2017.1350658
PMID:28738705
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6009881/
Abstract

A set of new sulfurated drug hybrids, mainly derived from caffeic and ferulic acids and rosmaricine, has been synthesized and their ability to inhibit both STAT3 and NF-κB transcription factors have been evaluated. Results showed that most of the new hybrid compounds were able to strongly and selectively bind to STAT3, whereas the parent drugs were devoid of this ability at the tested concentrations. Some of them were also able to inhibit the NF-κB transcriptional activity in HCT-116 cell line and inhibited HCT-116 cell proliferation in vitro with IC in micromolar range, thus suggesting a potential anticancer activity. Taken together, our study described the identification of new derivatives with dual STAT3/NF-κB inhibitory activity, which may represent hit compounds for developing multi-target anticancer agents.

摘要

已经合成了一组主要源自咖啡酸、阿魏酸和迷迭香碱的新型硫化药物杂化物，并评估了它们抑制STAT3和NF-κB转录因子的能力。结果表明，大多数新型杂化化合物能够强烈且选择性地与STAT3结合，而母体药物在测试浓度下没有这种能力。其中一些还能够抑制HCT-116细胞系中的NF-κB转录活性，并在体外以微摩尔范围的IC50抑制HCT-116细胞增殖，从而表明其具有潜在的抗癌活性。综上所述，我们的研究描述了具有双重STAT3/NF-κB抑制活性的新衍生物的鉴定，这些衍生物可能代表开发多靶点抗癌药物的先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/f6b2766c4c7d/IENZ_A_1350658_F0004_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/63d59eea27d7/IENZ_A_1350658_UF0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/03adc2bae850/IENZ_A_1350658_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/6aaa0d1bda3a/IENZ_A_1350658_F0002_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/1e8471392c1e/IENZ_A_1350658_F0003_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/12fc1ba3f349/IENZ_A_1350658_SCH0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/d3bb9a04c516/IENZ_A_1350658_SCH0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/bf520bef3241/IENZ_A_1350658_SCH0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/0eab73b666af/IENZ_A_1350658_SCH0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/f6b2766c4c7d/IENZ_A_1350658_F0004_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/63d59eea27d7/IENZ_A_1350658_UF0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/03adc2bae850/IENZ_A_1350658_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/6aaa0d1bda3a/IENZ_A_1350658_F0002_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/1e8471392c1e/IENZ_A_1350658_F0003_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/12fc1ba3f349/IENZ_A_1350658_SCH0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/d3bb9a04c516/IENZ_A_1350658_SCH0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/bf520bef3241/IENZ_A_1350658_SCH0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/0eab73b666af/IENZ_A_1350658_SCH0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db62/6009881/f6b2766c4c7d/IENZ_A_1350658_F0004_B.jpg

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