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探索新型香豆素连接的双三氮唑：诱导人胰腺癌细胞凋亡、抗菌作用及分子模拟研究。

Exploring Novel Coumarin-Tethered Bis-Triazoles: Apoptosis Induction in Human Pancreatic Cancer Cells, Antimicrobial Effects, and Molecular Modelling Investigations.

机构信息

School of Chemistry and Physics, University of KwaZulu-Natal, P/Bag X54001, Westville, Durban, 4000, South Africa.

Department of Pharmacology, Penn State College of Medicine, Penn State Cancer Institute, CH72, 500 University Drive, Hershey, PA 17033, USA.

出版信息

ChemMedChem. 2024 Nov 18;19(22):e202400297. doi: 10.1002/cmdc.202400297. Epub 2024 Sep 9.

DOI:10.1002/cmdc.202400297
PMID:39015094
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11581422/
Abstract

In the present study, we identified that two representative compounds (7 c and 9 f) of our newly synthesized coumarin-tagged bis-triazoles induced apoptosis in human pancreatic cells (PANC-1) by caspase 3/7mediated pathway. Both 7 c and 9 f (IC=7.15±1.19 and 6.09±0.79 μM, respectively) were found to be ~100 times superior against PANC-1 as compared to the standard drug Gemcitabine (IC=>500 μM), without showing any toxicity to the normal pancreatic epithelial cells (H6C7). Molecular docking studies further endorsed them as potential pancreatic cancer therapeutics due to their strong hydrogen bonding interactions with the epidermal growth factor receptor (EGFR) enzyme, which is overexpressed in cancerous cells including pancreatic cancer. Additionally, these compounds also showed moderate inhibitory activity against a panel of microbial strains. Overall, our findings reveal that the coumarin hybrids 7 c and 9 f are viable chemotypes to be adopted as templates for the development of new anticancer drugs, particularly against pancreatic cancer.

摘要

在本研究中，我们鉴定出两种我们新合成的香豆素标记双三唑代表化合物（7c 和 9f）通过半胱天冬酶 3/7 介导的途径诱导人胰腺细胞（PANC-1）凋亡。7c 和 9f（IC=7.15±1.19 和 6.09±0.79 μM，分别）被发现对 PANC-1 的活性比标准药物吉西他滨（IC=>500 μM）高约 100 倍，而对正常胰腺上皮细胞（H6C7）没有显示出任何毒性。分子对接研究进一步证明它们是潜在的胰腺癌治疗药物，因为它们与表皮生长因子受体（EGFR）酶具有很强的氢键相互作用，而这种酶在包括胰腺癌在内的癌细胞中过度表达。此外，这些化合物对一系列微生物菌株也表现出中等抑制活性。总的来说，我们的研究结果表明，香豆素杂合体 7c 和 9f 是可行的化学型，可作为开发新抗癌药物的模板，特别是针对胰腺癌。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/61f165c7ebc1/CMDC-19-e202400297-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/c378b3726700/CMDC-19-e202400297-g023.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/555db95c4b69/CMDC-19-e202400297-g016.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/877e2ac44fc9/CMDC-19-e202400297-g015.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/662b9dabb65c/CMDC-19-e202400297-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/aee689888baa/CMDC-19-e202400297-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/a1d49af47927/CMDC-19-e202400297-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/61f165c7ebc1/CMDC-19-e202400297-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/c378b3726700/CMDC-19-e202400297-g023.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/555db95c4b69/CMDC-19-e202400297-g016.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/877e2ac44fc9/CMDC-19-e202400297-g015.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/662b9dabb65c/CMDC-19-e202400297-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/aee689888baa/CMDC-19-e202400297-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/a1d49af47927/CMDC-19-e202400297-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b61/11581422/61f165c7ebc1/CMDC-19-e202400297-g008.jpg

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本文引用的文献

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