In vitro cytotoxic investigation of some synthesized 1,6-disubstituted-1-azacoumarin derivatives as anticancer agents

被引：4
作者：
Ali Barakat, Lamiaa Abellatef [1 ]
El-Deen, Ibrahim Mohy [1 ]
El-Zend, Manar Abdo [1 ]
El-Behery, Mohammed [1 ]
机构：
[1] Port Said Univ, Fac Sci, Dept Chem, Port Said 42511, Egypt
来源：
FUTURE MEDICINAL CHEMISTRY | 2023年 / 15卷 / 24期
关键词：
anticancer; azacoumarin; Bax/Bcl2; caspase; 3/7; cytotoxicity; docking; MCF-7; APOPTOSIS; COUMARIN; DOCKING; CANCER;
D O I：
10.4155/fmc-2023-0260
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Aims: In this study, novel synthesized 1,6-disubstituted-1-azacoumarin-3-carboxylic acid derivatives were designed, synthesized and evaluated as potential anticancer agents. Materials & methods: The cytotoxicity of novel 1-azacoumarin-3-carboxylic acid derivatives was tested using an MTT assay. High potency was shown by DNA flow cytometry on MCF-7 cells for compound 3b. In addition, topoisomerase II beta, caspase 3/7, Bax and Bcl-2 enzymes were used to study apoptotic activity. In the same studies, molecular docking analysis assessed activity. Results & conclusion: Cytotoxicity screening identified multiple bioactive compounds, especially compound 3b. Analysis of DNA flow cytometry revealed that compound 3b exhibited cell cycle arrest. Compound 3b had an increase in the expression of Bax/Bcl-2 ratio and caspase 3/7, and a decrease in topoisomerase II beta enzyme inhibition.
引用
收藏
页码：2289 / 2307
页数：19
相关论文
共 51 条
[1]   Characterization of Annexin V Fusion with the Superfolder GFP in Liposomes Binding and Apoptosis Detection [J].
Abbady, Abdul Qader ;
Twair, Aya ;
Ali, Bouthaina ;
Murad, Hossam .
FRONTIERS IN PHYSIOLOGY, 2017, 8
[2]   In Vitro Anticancer Evaluation of Some Synthesized 2H-Quinolinone and Halogenated 2H-Quinolinone Derivatives as Therapeutic Agents [J].
Abd El-Aziz, Rahma M. ;
Zaki, Islam ;
El-Deen, Ibrahim M. ;
Abd-Rahman, Marwa S. ;
Mohammed, Faten Z. .
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 2020, 20 (18) :2304-2315
[3]   Design, synthesis, and cytotoxic screening of novel azole derivatives on hepatocellular carcinoma (HepG2 Cells) [J].
Abdelhameid, Mohammed K. ;
Zaki, Islam ;
Mohammed, Manal R. ;
Mohamed, Khaled O. .
BIOORGANIC CHEMISTRY, 2020, 101
[4]   Design, Synthesis and Anticancer Evaluation of Substituted Cinnamic Acid Bearing 2-Quinolone Hybrid Derivatives [J].
Abu Almaaty, Ali H. ;
Elgrahy, Nermeen A. ;
Fayad, Eman ;
Abu Ali, Ola A. ;
Mahdy, Ahmed R. E. ;
Barakat, Lamiaa A. A. ;
El Behery, Mohammed .
MOLECULES, 2021, 26 (16)
[5]   Pyrazolo[3,4-d]pyrimidine derivatives as EGFRT790M and VEGFR-2 dual TK inhibitors: Design, synthesis, molecular docking, ADMET profile and anticancer evaluations [J].
Adel, Dina ;
El-Adl, Khaled ;
Nasr, Tamer ;
Sakr, Tamer M. ;
Zaghary, Wafaa .
JOURNAL OF MOLECULAR STRUCTURE, 2023, 1291
[6]   Coumarins and Coumarin-Related Compounds in Pharmacotherapy of Cancer [J].
Akkol, Esra Kupeli ;
Genc, Yasin ;
Karpuz, Busra ;
Sobarzo-Sanchez, Eduardo ;
Capasso, Raffaele .
CANCERS, 2020, 12 (07) :1-25
[7]   Design, Synthesis, and Investigation of Cytotoxic Activity of cis-Vinylamide-Linked Combretastatin Analogues as Potential Anticancer Agents [J].
Al-Warhi, Tarfah ;
Alqahtani, Leena S. ;
Alsharif, Ghadi ;
Abualnaja, Matokah ;
Abu Ali, Ola A. ;
Qahl, Safa H. ;
Althagafi, Hussam Awwadh E. ;
Alharthi, Fahad ;
Jafri, Ibrahim ;
Elsaid, Fahmy G. ;
Shati, Ali A. ;
Aloufi, Salman ;
Fayad, Eman ;
Zaki, Islam ;
Morcoss, Martha M. .
SYMMETRY-BASEL, 2022, 14 (10)
[8]   Cell cycle regulation and anticancer drug discovery [J].
Bai, Jingwen ;
Li, Yaochen ;
Zhang, Guojun .
CANCER BIOLOGY & MEDICINE, 2017, 14 (04) :348-362
[9]   Synthesis and anticancer evaluation of some coumarin and azacoumarin derivatives [J].
Bakare, Safyah B. .
POLISH JOURNAL OF CHEMICAL TECHNOLOGY, 2021, 23 (02) :27-34
[10]  
Behery ME., 2023, J MOL STRUCT, V1294
123456