Synthesis of Analogs of 2-Methoxyestradiol with Enhanced Inhibitory Effects on Tubulin Polymerization and Cancer Cell Growth

1997 ◽  
Vol 40 (15) ◽  
pp. 2323-2334 ◽  
Author(s):  
Mark Cushman ◽  
Hu-Ming He ◽  
John A. Katzenellenbogen ◽  
Ravi K. Varma ◽  
Ernest Hamel ◽  
...  
ChemInform ◽  
2010 ◽  
Vol 28 (48) ◽  
pp. no-no
Author(s):  
M. CUSHMAN ◽  
H.-M. HE ◽  
J. A. KATZENELLENBOGEN ◽  
R. K. VARMA ◽  
E. HAMEL ◽  
...  

2018 ◽  
Vol 83 (9) ◽  
pp. 2369-2374 ◽  
Author(s):  
Karnell L. Grimes ◽  
Connor M. Stuart ◽  
Justin J. McCarthy ◽  
Baljinder Kaur ◽  
Emilio J. Cantu ◽  
...  

2002 ◽  
Vol 74 (8) ◽  
pp. 1469-1477 ◽  
Author(s):  
Yoav Sharoni ◽  
Michael Danilenko ◽  
Shlomo Walfisch ◽  
Hadar Amir ◽  
Amit Nahum ◽  
...  

There is extensive evidence that high intake of fruits and vegetables is associated with decreased risk of many types of cancers. Thus, it is widely accepted that diet changes are a powerful means to prevent cancer. Although there is a growing interest in the role of the tomato carotenoid lycopene in cancer prevention and treatment, we hypothesize that a single micronutrient cannot replace the power of the concerted action of multiple agents derived from a diet rich in fruits and vegetables. Indeed, we found that lycopene can synergize with other phytonutrients in the inhibition of cancer cell growth. The mechanism underlying the inhibitory effects of lycopene and other carotenoids involves interference in several pathways related to cancer cell proliferation and includes changes in the expression of many proteins participating in these processes, such as connexins, cyclins, cyclin-dependent kinases, and their inhibitors. These changes in protein expression suggest that the initial effect involves modulation of transcription by ligand-activated nuclear receptors or by other transcription factors. It is feasible to suggest that carotenoids and their oxidized derivatives interact with a network of transcription systems that are activated by different ligands at low affinity and specificity and that this activation leads to the synergistic inhibition of cell growth.


2000 ◽  
Vol 118 (4) ◽  
pp. A1409
Author(s):  
Amy T. Rose ◽  
Tracy Heisler ◽  
Shirin Towfigh ◽  
Natalie Simon ◽  
David W. McFadden

2020 ◽  
Vol 16 ◽  
Author(s):  
Syed Nasir Abbas Bukhari ◽  
Nasser Hadal Alotaibi ◽  
Waqas Ahmad ◽  
Khalid Saad Alharbi ◽  
Mohamed A. Abdelgawad ◽  
...  

Background: Ligustrazine and chalcones have been reported previously for various biological activities including anticancer effects. Objectives: Based on the multitargeted biological activities approach of ligustrazine based chalcones, in current study 18 synthetic ligustrazine-containing α, β-unsaturated carbonyl-based 1, 3-Diphenyl-2-propen-1-one derivatives were evaluated for their inhibitory effects on growth of five different types of cancer cells. Methods: All compounds were evaluated for anticancer effects on various cancer cell lines by propidium iodide fluorescence assay and various other assays were performed for mechanistic studies. Results: Majority of compounds exhibited strong inhibition of cancer cells especially synthetic compounds 4a and 4b bearing 1-Pyridin-3-yl-ethanone as a ketone moiety in main structural backbone were found most powerful inhibitors of cancer cell growth. Most active 9 compounds among whole series were selected for further studies related to different cancer targets including EGFR TK kinases, tubulin polymerization, KAF and BRAFV600E. Conclusion: Synthetic derivatives including 4a-b and 5a-b showed multitarget approach and showed strong inhibitory effects on EGFR, FAK and BRAF while three compounds including 3e bearing methoxy substitution, 4a and 4b with 1- pyridin-3-yl-ethanone moiety showed the inhibition of tubulin polymerization.


2010 ◽  
Vol 62 (4) ◽  
pp. 349-355 ◽  
Author(s):  
Jinling Luan ◽  
Huiying Duan ◽  
Qian Liu ◽  
Kazumi Yagasaki ◽  
Guoying Zhang

2010 ◽  
Vol 6 (3) ◽  
pp. 114-122 ◽  
Author(s):  
Chisato Ishimaru ◽  
Toshifumi Takeuchi ◽  
Fumio Sugawara ◽  
Hiromi Yoshida ◽  
Yoshiyuki Mizushina

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