Coumarin-Piperazine Tethered 1,2,3-Triazoles: EGFR Targeting Anti-Breast Cancer Evaluation and Molecular Docking Studies

被引：3

作者：

Gangadhar, Kotni Hari ^{[1
]}

Benarjee, Velaga ^{[2
]}

Ratnamala, Annapragada ^{[1
]}

机构：

[1] GITAM Univ, Dept Chem, Hyderabad Campus, Hyderabad, Telangana, India

[2] Andhra Univ, Dept Inorgan & Analyt Chem, Visakhapatnam, Andhra Pradesh, India

来源：

POLYCYCLIC AROMATIC COMPOUNDS | 2024年 / 44卷 / 08期

关键词：

Anti-breast cancer activity; anti-EGFR activity; coumarin; piperazine; 1,2,3-triazole; ANTICANCER ACTIVITY EVALUATION; BIOLOGICAL EVALUATION; DERIVATIVES; DESIGN; HYBRIDS; ANALOGS; AGENTS;

D O I：

10.1080/10406638.2023.2265026

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

We synthesized a new series of coumarin-piperazine 1,2,3-triazole hybrids (7a-7n) and screened for their in vitro anti-breast cancer activity against MCF-7, MDA-MB-468, and MDA-MB-231 cancer cell lines. The results revealed that compound 7f showed superior activity against all cell lines than the standard drug 5-fluorouracil. As well, compounds 7e, 7h, and 7k showed greater activity against MCF-7 than the positive control. Furthermore, 7f and 7h showed higher potency in inhibiting tyrosine kinase epidermal growth factor receptor (EGFR) than the standard drug erlotinib. Finally, in silico molecular docking studies on EGFR (PDB ID-4HJO) revealed that compounds 7e, 7f, 7h, and 7k possess good binding energies and inhibition constants as compared to erlotinib.

引用

页码：5487 / 5503

页数：17

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