Synthesis of 1,3,4-Oxa(Thia)Diazole Derivatives of Amidomethylcytisine

Ismailova, D. S.; Ziyaev, A. A.; Левкович, М. Г.; Toshmurodov, Turdibek

doi:10.1007/s10600-018-2489-6

Chem Nat Compd

2018

DOI: 10.1007/s10600-018-2489-6

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Synthesis of 1,3,4-Oxa(Thia)Diazole Derivatives of Amidomethylcytisine

D. S. Ismailova

A. A. Ziyaev

М. Г. Левкович

et al.

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Cited by 3 publications

References 7 publications

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Design, Synthesis, Biological Evaluation and Molecular Docking Study of New 1,3,4‐Thiadiazole‐Based Compounds as EGFR Inhibitors

Serag,

Tawfik,

Eisa

et al. 2024

Drug Development Research

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Five series of new 1,3,4‐thiadiazole hybrids were designed and synthesized as promising EGFR inhibitors. Three human cancer cell lines were employed for testing each hybrid's in vitro antiproliferative efficacy; colon HCT‐116, liver HepG‐2 and breast MCF‐7 using MTT assay. Comparing compound 9a to the reference doxorubicin, 9a shown superior activity to that of Dox with respect to MCF‐7 (IC50 3.31 µM) while being secure for normal cells WI‐38 (IC50 = 43.99 µM). Further evaluation of the EGFR inhibitory activity of the most active candidates—4a, 6b, 8b, 9a, and 9 d—was performed. Of them, compounds 9a and 8b demonstrated the highest IC50 values, 0.08 and 0.15 µM, respectively, relative to the reference gefitinib (IC50 = 0.04 µM). Subsequent mechanistic analysis of compound 9a revealed a notable 14.24‐fold increase in overall apoptosis and a 28.92% cell cycle arrest at G2/M. Additionally, research on apoptosis demonstrated that it triggered the mitochondrial apoptotic pathway. In MCF‐7 cells, it also led to an increase in ROS buildup. For the most powerful EGFR inhibitors, 9a and 8b, a molecular docking research was conducted, and all of the findings agreed with the biological findings.

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Design, Synthesis, Biological Evaluation and Molecular Docking Study of New 1,3,4‐Thiadiazole‐Based Compounds as EGFR Inhibitors

Serag,

Tawfik,

Eisa

et al. 2024

Drug Development Research

View full text Add to dashboard Cite

show abstract

Solvent-free synthesis of cytisine-thienopyrimidinone conjugates via transannulation of 1H-tetrazoles: Crystal and molecular structure, docking studies and screening for anticancer activity

Pokhodylo

Shyyka

Slyvka

et al. 2021

Journal of Molecular Structure

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Advances on the Bioactivities, Total Synthesis, Structural Modification, and Structure-Activity Relationships of Cytisine Derivatives

Huang

2020

MRMC

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Cytisine is a quinolizidine alkaloid isolated from various Leguminosae plants. Cytisine and its derivatives exhibit a broad range of biological properties, such as smoking cessation aid, antidepressant, neuroprotective, nootropic, anticancer, antiviral, antiparasitic, antidiabetic, insecticidal, and nematicidal activities. In this review, the progress of cytisine and its derivatives in regard to bioactivities, total synthesis, structural modifications focusing on their N-12 position and lactam ring is reported. Additionally, the structure-activity relationships of cytisine and its derivatives are also discussed.

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Synthesis of 1,3,4-Oxa(Thia)Diazole Derivatives of Amidomethylcytisine

Cited by 3 publications

References 7 publications

Design, Synthesis, Biological Evaluation and Molecular Docking Study of New 1,3,4‐Thiadiazole‐Based Compounds as EGFR Inhibitors

Design, Synthesis, Biological Evaluation and Molecular Docking Study of New 1,3,4‐Thiadiazole‐Based Compounds as EGFR Inhibitors

Solvent-free synthesis of cytisine-thienopyrimidinone conjugates via transannulation of 1H-tetrazoles: Crystal and molecular structure, docking studies and screening for anticancer activity

Advances on the Bioactivities, Total Synthesis, Structural Modification, and Structure-Activity Relationships of Cytisine Derivatives

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