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新型氰基嘧啶衍生物作为潜在的抗癌药物。

Novel Cyanopyrimidine Derivatives as Potential Anticancer Agents.

作者信息

Abd El-Hameed Rania H, Aly Omnia, Mohamed Mariem E, Gharib Amal F, Mohamed Mosaad S, Ali Ashraf, Khoder Zainab M, Taha Heba, Fatahala Samar S

机构信息

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Cairo 11795, Egypt.

Medical Biochemistry Department, National Research Centre, Dokki 12622, Egypt.

出版信息

Molecules. 2025 Mar 25;30(7):1453. doi: 10.3390/molecules30071453.

DOI:10.3390/molecules30071453
PMID:40286038
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11990787/
Abstract

The Bcl-2 family's anti-apoptotic proteins, particularly Mcl-1, offer a viable avenue for cancer treatment since cancer cells can undergo apoptosis when their selective suppression occurs. Mcl-1 is essential for controlling the advancement of the cell cycle, as well as apoptosis. There is a constant clinical need for more potent treatments for breast and ovarian malignancies, even with advancements in the discovery of anticancer drugs. By synthesizing cyanopyrimidine derivatives that demonstrate both dual inhibitory activity against Mcl-1 and Bcl-2, and successful cell cycle arrest, our research seeks to contribute to the development of innovative therapeutic medicines. We created a number of new 6-substituted cyanopyrimidines and tested their anticancer effects on SKOV-3 and MCF-7 cell lines as well as apoptosis and cell cycle arrest assays.

摘要

Bcl-2家族的抗凋亡蛋白,尤其是Mcl-1,为癌症治疗提供了一条可行途径,因为当癌细胞的选择性抑制发生时,它们会发生凋亡。Mcl-1对于控制细胞周期进程以及凋亡至关重要。即使在抗癌药物发现方面取得了进展,临床上仍持续需要更有效的乳腺癌和卵巢癌治疗方法。通过合成对Mcl-1和Bcl-2均具有双重抑制活性且能成功使细胞周期停滞的氰基嘧啶衍生物,我们的研究旨在为创新治疗药物的开发做出贡献。我们制备了多种新型6-取代氰基嘧啶,并测试了它们对SKOV-3和MCF-7细胞系的抗癌作用以及凋亡和细胞周期停滞分析。

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