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融合苯并[ ]色烯并[2,3-]嘧啶对人乳腺癌 MCF-7 细胞系的合成、抗癌活性、细胞周期阻滞、凋亡诱导及对接研究。

Synthesis, Anti-Cancer Activity, Cell Cycle Arrest, Apoptosis Induction, and Docking Study of Fused Benzo[]chromeno[2,3-]pyrimidine on Human Breast Cancer Cell Line MCF-7.

机构信息

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

Department of Chemistry, The State University of New York at Buffalo, New York, NY 14260, USA.

出版信息

Molecules. 2024 Oct 4;29(19):4697. doi: 10.3390/molecules29194697.

Abstract

Breast cancer is the predominant form of cancer among women and ranks as the second most prevalent cancer globally, affecting both developed and less developed countries. Presently, accessible cancer treatment methods either employ recently created, secure, and efficient chemotherapeutic medications or directly target innovative pathways that cause apoptosis. One of the indirect strategies for treating this fatal illness has mostly depended on its essential role in cell cycle arrest and apoptosis induction, as well as the antagonistic interaction between the Bcl-2 and Mcl-1 proteins, in order to avert major health repercussions. We reported that newly synthesized fused chromenopyrimidines ( and ) showed potential cell cycle arrest and dual Bcl-2 and Mcl-1 inhibitory characteristics. Bcl-2 and Mcl-1 were the targets of a molecular docking procedure. The previous docking results are in line with the biological data and suggest that may have promising anti-cancer activity.

摘要

乳腺癌是女性中最常见的癌症形式,也是全球第二大常见癌症,影响着发达国家和欠发达国家。目前,可获得的癌症治疗方法要么使用最近开发的、安全有效的化疗药物,要么直接针对导致细胞凋亡的创新途径。治疗这种致命疾病的间接策略之一主要依赖于其在细胞周期阻滞和凋亡诱导中的重要作用,以及 Bcl-2 和 Mcl-1 蛋白之间的拮抗相互作用,以避免重大的健康影响。我们报道了新合成的融合色烯嘧啶(和)显示出潜在的细胞周期阻滞和双重 Bcl-2 和 Mcl-1 抑制特性。Bcl-2 和 Mcl-1 是分子对接程序的靶点。以前的对接结果与生物学数据一致,并表明可能具有有前途的抗癌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15cf/11478142/ce4ab7812851/molecules-29-04697-g001.jpg

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