Aminocyanopyridines as anti‐lung cancer agents by inhibiting the STAT3 pathway

Xu, Linhao; Qiu, Sensen; Yang, Lehe; Xu, Haowen; Liu, Xu; Fan, Shuli; Cui, Ri; Fu, Weitao; Zhao, Chengguang; Shen, Liqun; Wang, Liangxing; Huang, Xiaoying

doi:10.1002/mc.23038

Cited by 7 publications

(5 citation statements)

References 33 publications

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“…To maintain conformational stability, compound 32 also forms two hydrogen bonds with residues Ser-63 and Glu-638. [27] STAT3 is considered to be a major oncogene in the development of colorectal cancer. [28] Therefore, inhibiting STAT3 seems to be a promising cancer treatment.…”

Section: Survivin Inhibitorsmentioning

confidence: 99%

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A review: Biological activities of novel cyanopyridine derivatives

Huang

2023

Archiv der Pharmazie

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The discovery of new therapeutic drugs is heavily reliant on the structural diversity and pharmacological properties of heterocyclic compounds. Pyridine heterocyclic‐related medicines, in particular, have garnered considerable attention due to their wide pharmacological activities and therapeutic effects. Among them, cyanopyridine derivatives have demonstrated diverse pharmacological effects. This review aims to systematically compile and discuss the diverse pharmacological effects of cyanopyridine derivatives. The review is divided into multiple sections, highlighting the biological activities of cyanide derivatives, with emphasis on anticancer, antimicrobial (i.e., antibacterial, insecticidal anticonvulsant, and antiviral activities), anticonvulsant, anti‐Alzheimer's, and enzyme inhibitory activities. Furthermore, the review emphasizes the interesting therapeutic potential of cyanopyridine derivatives as kinase inhibitors and cytotoxic agents, which are promising candidates for anticancer drug development. The relationship between structure and activity is also discussed, with molecular docking used to provide insights into the mechanism of action of these compounds.

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Section: Survivin Inhibitorsmentioning

confidence: 99%

“…To maintain conformational stability, compound 32 also forms two hydrogen bonds with residues Ser‐63 and Glu‐638. [ 27 ]…”

Section: Biological Activities Of Cyanopyridinesmentioning

confidence: 99%

A review: Biological activities of novel cyanopyridine derivatives

Huang

2023

Archiv der Pharmazie

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“…Aminocyanopyridines can inhibit cell proliferation and induce cell death in human cancer cells by inhibiting the STAT3 pathway 17. We next validated the effects of 3n on STAT3 signaling in three colorectal cancer cells.…”

Section: Resultsmentioning

confidence: 95%

“…There are relatively few reports on 3-amino-3-cyanopyridine compounds compared to 2-amino-3-cyanopyridine compounds, and there are few studies on the anti-tumor activity of such compounds 16. Our group has previously demonstrated that the aminocyanopyridines exhibit significant antitumor activity against lung cancers in vitro and in vivo 17. So we continued our previous studies to further design, synthesize and evaluate the in vitro anticancer activity of a series of aminocyanopyridines.…”

Section: Introductionmentioning

confidence: 96%

<p>Design, Synthesis, And Evaluation Of Cyanopyridines As Anti-Colorectal Cancer Agents Via Inhibiting STAT3 Pathway</p>

Shi

Qiu

et al. 2019

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BackgroundColorectal cancer is one of the common malignant tumors. Cyanopyridine and aminocyanopyridine having a carbon-nitrogen bond have been shown to have significant anticancer effects. STAT3 is a promising therapeutic target in multiple cancers. However, there are currently no effective STAT3 inhibitors in clinical practice for the treatment of colorectal cancer.Materials and methodsWe screened 27 cyanopyridines for their anticancer activity by cell viability. The HCT-116, RKO, and DLD-1 cell lines were used to evaluate the anti-colorectal cancer effect of 3n. Scratch experiments and colony formation assays were used for the assessment of cell migration and proliferation capacity. Phosphorylated STAT3, STAT3, MCL-1, and Survivin levels were assessed by Western blot analysis.ResultsIn this study, we synthesized 27 cyanopyridines and screened their anticancer activities in three human tumor cells, HCT-116, Hela229, and A375. We found that 2-amino-3-cyanopyridine 3n has better anticancer activity with IC50 values in the low micromolar range. Furthermore, 3n significantly inhibited the migration and colony formation of colorectal cancer cells. Mechanistically, 3n inhibited the expression of STAT3 phosphorylation in a dose- and time-dependent manner.Conclusion3n is worth of further investigations toward the discovery of STAT3 inhibitor as a drug candidate for cancer therapy.

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“…43 There are not many systems available that are more viable in terms of environmental protection and atom economy. Among the nitrogen heterocyclic compounds, aminocyanohydropyridine derivatives are important motifs for organic synthesis and are widely found in many natural products, having different biological activities such as antimicrobial agents, 44 anticancer agents, 45 psychotropic, 46 anti-allergenic, 46 anti-inflammatory, 46 and estrogenic activities, and MK-2 kinase inhibitors 7 (Fig. 1 compound I , II ).…”

Section: Introductionmentioning

confidence: 99%