Design, synthesis and anticancer evaluation of some novel 7-hydroxy-4-methyl-3-substituted benzopyran-2-one derivatives

被引：0
|
作者：
Abd El-Haleem, Akram H. [1 ]
Ellafy, Manar A. [1 ]
Abbas, Safinaz E-S [2 ]
El-Ashrey, Mohamed K. [2 ,3 ]
机构：
[1] Misr Univ Sci & Technol, Fac Pharm, Pharmaceut Chem Dept, PO 77, 6th October City, Giza, Egypt
[2] Cairo Univ, Fac Pharm, Pharmaceut Chem Dept, Kasr Elini St, Cairo 11562, Egypt
[3] King Salman Int Univ KSIU, Fac Pharm, Med Chem Dept, South Sinai 46612, Egypt
来源：
FUTURE MEDICINAL CHEMISTRY | 2024年 / 16卷 / 05期
关键词：
7-hydroxy-4-methyl-3-substituted benzopyran-2-ones; Akt-1; anticancer activity; benzopyran-2-one; PI3K; COUMARINS; CANCER;
D O I：
10.4155/fmc-2023-0294
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Aim: 22 derivatives of 7-hydroxy-4-methyl-3-substituted benzopyran-2-one were designed, synthesized and evaluated for their anticancer activity. Materials & methods: The prepared compounds were screened for their cytotoxicity against the MCF-7 breast cancer cell line. The best five were then evaluated against MCF10a to check their safety and then tested for their PI3K and Akt-1 inhibitory action. The best two derivatives were further analyzed through cell cycle analysis, caspase 3/7 activation, increasing BAX level and decreasing BCL-2. Docking and absorption, distribution, metabolism and excretion prediction studies were also performed. Results & conclusion: Compounds 3b, 3c, 3j, 7 and 8 were the most active. Compounds 3c and 8 showed remarkable inhibitory action against PI3K and Akt-1 enzymes, and both are promising candidates for treatment of breast cancer.
引用
收藏
页码：417 / 437
页数：21
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