Construction of indazolo[3,2-a]isoquinolines via [3 + 2] cycloaddition of benzynes

2019 ◽  
Vol 17 (40) ◽  
pp. 8963-8968 ◽  
Author(s):  
Yue-Kun Li ◽  
Ming-Xin Cui ◽  
Feng Sha ◽  
Qiong Li ◽  
Xin-Yan Wu
Keyword(s):  
Cancer Cells ◽  
Proliferative Activity ◽  
Diverse Range ◽  
Azomethine Imines

A [3 + 2] annulation protocol for the construction of N-substituted indazolo[3,2-a]isoquinolines starting from benzynes and C,N-cyclic azomethine imines was developed. A diverse range of indazolo[3,2-a]isoquinolines can be easily accessed, which show good anti-proliferative activity on cancer cells.

Synthesis, In-vitro and Docking Analysis of C-3 substituted Coumarin Analogues as Anticancer Agents C-3 Substituted Coumarins as Anticancer Agents

2020 ◽  
Vol 16 ◽  
Author(s):  
Anuradha Thakur ◽  
Kamalpreet Kaur ◽  
Praveen Sharma ◽  
Ramit Singla ◽  
Sandeep Singh ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Molecular Docking ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Anticancer Agents ◽  
Proliferative Activity ◽  
Binding Interaction ◽  
Diverse Range ◽  
Mcf 7 ◽  
Substituted Coumarins

Background: Breast cancer (BC) is a leading cause of cancer-related deaths in women next to skin cancer. Estrogen receptors (ERs) play an important role in the progression of BC. Current anticancer agents have several drawbacks such as serious side effects and the emergence of resistance to chemotherapeutic drugs. As coumarins possess minimum side effect along with multi-drug reversal activity, it has a tremendous ability to regulate a diverse range of cellular pathways that can be explored for selective anticancer activity. Objectives: Synthesis and evaluation of new coumarin analogues for anti-proliferative activity on human breast cancer cell line MCF-7 along with exploration of binding interaction of the compounds for ER-α target protein by molecular docking. Method: In this study, the anti-proliferative activity of C-3 substituted coumarins analogues (1-17) has been evaluated against estrogen receptor-positive MCF-7 breast cancer cell lines. Molecular interactions and ADME study of the compounds were analyzed by using Schrodinger software. Results: Among the synthesized analogues 12 and 13 show good antiproliferative activity with IC50 values 1and 1.3 µM respectively. Molecular docking suggests a remarkable binding pose of all the seventeen compounds. Compounds 12 and 13 were found to exhibit dock score of -4.10 kcal/mol and -4.38 kcal/mol respectively. Conclusion: Compounds 12 and 13 showed the highest activity followed by 1 and 5. ADME properties of all compounds were in the acceptable range. The active compounds can be taken for lead optimization and mechanistic interventions for their in vivo study in the future.

scholarly journals Phytochemical screening and anticancer activity of the aerial parts extract of Xanthium strumarium L. on HepG2 cancer cell line

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Hai Trieu Ly ◽  
Trieu Minh Truong ◽  
Thi Thu Huong Nguyen ◽  
Hoang Dung Nguyen ◽  
Yuxia Zhao ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Proliferative Activity ◽  
Herbal Medicines ◽  
Cancer Cell Line ◽  
Cancer Therapeutics ◽  
Ethanol Extract ◽  
Xanthium Strumarium ◽  
Aerial Parts ◽  
Dual Staining

Abstract Background Cancer is one of the most considerable concerns because of increasing the death rate all over the world. Recent studies have disclosed that plant extracts exhibit anticancer activity through various mechanisms. Xanthium strumarium has been used by Vietnamese in herbal medicines to support the medication of infirmities. This study is to consider the secondary metabolites, antioxidant and anticancer capacities of extract from the aerial parts (stems and leaves) of X. strumarium (AP-XS). Methods AP-XS was analyzed for the presence of phytochemicals via qualitative chemical tests and determined total polyphenol and flavonoid contents. DPPH (1,1-diphenyl-2-picrylhydrazyl) quenching assay and sulforhodamine B (SRB) assay were selected to investigate antioxidant capacity and anti-proliferative activity, respectively. Besides, acridine orange-ethidium bromide (AO-EB) dual staining was applied to evaluate the ability to induce apoptosis on HepG2 cancer cells. Results Results of present study indicated that AP-XS contains the main phytochemicals such as flavonoids, tannins, saponins, alkaloids, and triterpenes. Ethanol extract had highest content of polyphenol (84.86 mg gallic acid equivalent/g dry mass), and exhibited the great total antioxidant property (IC50 = 184.13 μg/mL) and anti-proliferative activity on HepG2 cancer cells (IC50 = 81.69 μg/mL). Furthermore, the characteristics of apoptosis including shrinkage of the cell and apoptotic bodies were found following 60 h of AP-XS extract treatment through AO-EB dual staining. Conclusion The data suggest that AP-XS extract had antioxidant potential and anti-proliferative effect. The anti-proliferative property was considered to have an association with a rising of apoptosis. These results were reliable for further research on X. strumarium as a source of phytochemicals with anticancer activity potential for cancer therapeutics.

scholarly journals Microbial Metabolites of Flavanols in Urine are Associated with Enhanced Anti-Proliferative Activity in Bladder Cancer Cells In Vitro

2021 ◽  
pp. 1-17
Author(s):  
Laura E. Griffin ◽  
Sarah E. Kohrt ◽  
Atul Rathore ◽  
Colin D. Kay ◽  
Magdalena M. Grabowska ◽  
...  
Keyword(s):  
Bladder Cancer ◽  
Cancer Cells ◽  
Proliferative Activity ◽  
Microbial Metabolites ◽  
Bladder Cancer Cells

Survivin Gene Expression Positively Correlates with Proliferative Activity of Cancer Cells in Esophageal Cancer

Tumor Biology ◽  
2003 ◽  
Vol 24 (1) ◽  
pp. 40-45 ◽  
Author(s):  
Masahide Ikeguchi ◽  
Ken-ichi Yamaguchi ◽  
Nobuaki Kaibara
Keyword(s):  
Gene Expression ◽  
Esophageal Cancer ◽  
Cancer Cells ◽  
Proliferative Activity ◽  
Survivin Gene

scholarly journals Phytochemical Properties and Anti-Proliferative Activity of Olea europaea L. Leaf Extracts against Pancreatic Cancer Cells

Molecules ◽  
2015 ◽  
Vol 20 (7) ◽  
pp. 12992-13004 ◽  
Author(s):  
Chloe Goldsmith ◽  
Quan Vuong ◽  
Elham Sadeqzadeh ◽  
Costas Stathopoulos ◽  
Paul Roach ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Cancer Cells ◽  
Olea Europaea ◽  
Proliferative Activity ◽  
Leaf Extracts ◽  
Olea Europaea L ◽  
Pancreatic Cancer Cells ◽  
Olea Europaéa
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