New pyrimidines and triazolopyrimidines as antiproliferative and antioxidants with cyclooxygenase-1/2 inhibitory potential

2019 ◽  
Vol 11 (13) ◽  
pp. 1583-1603
Author(s):  
Ashraf M Omar ◽  
Heba A Abd El Razik ◽  
Aly A Hazzaa ◽  
Maryam AZ El-Attar ◽  
Maha A El Demellawy ◽  
...  
Keyword(s):  
Free Radicals ◽  
Inhibitory Activity ◽  
Docking Studies ◽  
Cyclooxygenase 1 ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Cox 2 ◽  
Inhibitory Potential ◽  
Cox 1 ◽  
Mcf 7

Aim: Cyclooxygenase-2 (COX-2) inhibition and scavenging-free radicals are important targets in cancer treatment. Materials & methods: Sulfanylpyrimidines and triazolopyrimidines were synthesized and evaluated as anticancer and antioxidant COX-1/2 inhibitors. Results: Compound 7 showed the same growth inhibitory activity as 5-fluorouracil against MCF-7. Compound 6f displayed broad-spectrum anticancer activity against the four tested cancer cell lines. Compounds 5b, 6a, 6c, 6d and 8 were found to be more active antioxidants than trolox. Compounds 6a, 6c, 6f and 8 revealed high COX-2 inhibitory activity and selectivity, which was confirmed by docking studies. Conclusion: Compound 6f could be considered as promising anticancer and antioxidant structural lead with COX-2 inhibition that deserve further derivatization and investigation.

scholarly journals Chlorinated cobalt alkyne complexes derived from acetylsalicylic acid as new specific antitumor agents

2018 ◽  
Vol 47 (12) ◽  
pp. 4341-4351 ◽  
Author(s):  
Victoria Obermoser ◽  
Daniel Baecker ◽  
Carina Schuster ◽  
Valentin Braun ◽  
Brigitte Kircher ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Tumor Cell Lines ◽  
Growth Inhibitory ◽  
Cox 2 ◽  
Alkyne Complexes ◽  
Inhibitory Potential ◽  
Cox 2 Inhibitors ◽  
Ht 29 ◽  
Cox 1 ◽  
Mcf 7

Chlorine-substituted [(prop-2-ynyl)-2-acetoxybenzoate]dicobalthexacarbonyl complexes are selective COX-2 inhibitors with growth-inhibitory potential against COX-1/2 containing MDA-MB-231 and HT-29 tumor cell lines. The metabolic activity of non-tumorigenic HS-5 cells and COX-1/2-independent MCF-7 cells is not influenced.

New indomethacin analogs as selective COX‐2 inhibitors: Synthesis, COX‐1/2 inhibitory activity, anti‐inflammatory, ulcerogenicity, histopathological, and docking studies

2020 ◽  
Author(s):  
Khaled R. A. Abdellatif ◽  
Eman K. A. Abdelall ◽  
Heba A. H. Elshemy ◽  
El‐Shaymaa El‐Nahass ◽  
Maha M. Abdel‐Fattah ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Docking Studies ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Cox 1

Obtusifoliol related steroids from Euphorbia sogdiana with cell growth inhibitory activity and apoptotic effects on breast cancer cells (MCF-7 and MDA-MB231)

Steroids ◽  
2016 ◽  
Vol 115 ◽  
pp. 90-97 ◽  
Author(s):  
Mahmoud Aghaei ◽  
Zeinab Yazdiniapour ◽  
Mustafa Ghanadian ◽  
Behzad Zolfaghari ◽  
Virginia Lanzotti ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Growth ◽  
Cancer Cells ◽  
Inhibitory Activity ◽  
Breast Cancer Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Apoptotic Effects ◽  
Mcf 7

scholarly journals In vitro Anti-inflammatory Activity of Ligustrum vulgare Extracts and Their Analytical Characterization

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Anna Macková ◽  
Pavel Mučaji ◽  
Ute Widowitz ◽  
Rudolf Bauer
Keyword(s):  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Neutrophil Granulocytes ◽  
Cyclooxygenase 1 ◽  
Ligustrum Vulgare ◽  
China And Japan ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Interest in the anti-inflammatory effects of Ligustrum vulgare L., which has been used traditionally in China and Japan prompted us to determine anti-inflammatory effects of the plant's compounds in leukocytes. The leaves of L. vulgare were used to prepare a decoction which was successively extracted with organic solvents (dichloromethane (DCM), n-butanol, ethyl acetate) using liquid-liquid partition. Extracts were tested for inhibition of LTB4, resp. PGE2 biosynthesis. Each extract was evaluated for its in vitro cyclooxygenase-1/2 (COX-1/2) inhibitory activity using assays with purified COX-1 and COX-2 enzymes, as well as for their LTB4 formation inhibitory activity using an assay with activated human neutrophil granulocytes. All extracts reported inhibitory actions against COXs in comparison with the synthetic inhibitors NS-398 (IC50 = 2.6 μM) and indomethacin (IC50 = 0.9 μM). The dichloromethane extract of privet leaves showed a considerable inhibitory effect against COX-1 and COX-2 enzyme activity. The DCM extract revealed 2.7 times higher inhibitory activity against LTB4 formation in comparison with the known specific LT inhibitor zileuton (IC50 = 5.0 μM). Additionally, oleuropein and echinacoside were detected by HPLC-DAD and LC-MS in the Ligustrum vulgare leaves. Both compounds exhibited weak inhibitory activity on cyclooxygenases and leukotriene formation.

scholarly journals Inhibitory Mechanisms of Lusianthridin on Human Platelet Aggregation

2021 ◽  
Vol 22 (13) ◽  
pp. 6846
Author(s):  
Hla Nu Swe ◽  
Boonchoo Sritularak ◽  
Ponlapat Rojnuckarin ◽  
Rataya Luechapudiporn
Keyword(s):  
Arachidonic Acid ◽  
Platelet Aggregation ◽  
Adenosine Diphosphate ◽  
Docking Studies ◽  
Secondary Wave ◽  
Inhibitory Effects ◽  
Antiplatelet Aggregation ◽  
Cyclooxygenase 1 ◽  
Cox 2 ◽  
Cox 1

Lusianthridin is a phenanthrene derivative isolated from Dendrobium venustum. Some phenanthrene compounds have antiplatelet aggregation activities via undefined pathways. This study aims to determine the inhibitory effects and potential mechanisms of lusianthridin on platelet aggregation. The results indicated that lusianthridin inhibited arachidonic acid, collagen, and adenosine diphosphate (ADP)-stimulated platelet aggregation (IC50 of 0.02 ± 0.001 mM, 0.14 ± 0.018 mM, and 0.22 ± 0.046 mM, respectively). Lusianthridin also increased the delaying time of arachidonic acid-stimulated and the lag time of collagen-stimulated and showed a more selective effect on the secondary wave of ADP-stimulated aggregations. Molecular docking studies revealed that lusianthridin bound to the entrance site of the cyclooxygenase-1 (COX-1) enzyme and probably the active region of the cyclooxygenase-2 (COX-2) enzyme. In addition, lusianthridin showed inhibitory effects on both COX-1 and COX-2 enzymatic activities (IC50 value of 10.81 ± 1.12 µM and 0.17 ± 1.62 µM, respectively). Furthermore, lusianthridin significantly inhibited ADP-induced suppression of cAMP formation in platelets at 0.4 mM concentration (p < 0.05). These findings suggested that possible mechanisms of lusianthridin on the antiplatelet effects might act via arachidonic acid-thromboxane and adenylate cyclase pathways.

Cationic liposomes as efficient nanocarriers for the drug delivery of an anticancer cholesterol-based ruthenium complex

2015 ◽  
Vol 3 (15) ◽  
pp. 3011-3023 ◽  
Author(s):  
Giuseppe Vitiello ◽  
Alessandra Luchini ◽  
Gerardino D'Errico ◽  
Rita Santamaria ◽  
Antonella Capuozzo ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cancer Cells ◽  
Inhibitory Activity ◽  
Ruthenium Complex ◽  
Human Cancer ◽  
High Growth ◽  
Human Cancer Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Mcf 7

Cationic nanovectors loaded with Ru-based nucleolipids exert a high growth-inhibitory activity against human cancer cells (MCF-7 (A), WiDr (B), and HeLa (C)).

Troglitazone enhances tamoxifen-induced growth inhibitory activity of MCF-7 cells

2008 ◽  
Vol 377 (1) ◽  
pp. 242-247 ◽  
Author(s):  
Hong-Nu Yu ◽  
Eun-Mi Noh ◽  
Young-Rae Lee ◽  
Si-Gyun Roh ◽  
Eun-Kyung Song ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Mcf 7
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