Semi-synthesis and anti-lung cancer activity evaluation of aryl dihydrothiazol acyl podophyllotoxin ester derivatives

RSC Advances ◽  
2015 ◽  
Vol 5 (35) ◽  
pp. 27775-27784 ◽  
Author(s):  
Hong-Yan Lin ◽  
Li-Fei Bai ◽  
Fang Wang ◽  
Xun Wu ◽  
Lu-Jing Han ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Anticancer Agent ◽  
Tubulin Polymerization ◽  
Inhibition Effect ◽  
Activity Evaluation ◽  
Podophyllotoxin Derivatives ◽  
Cancer Activity

S12, the best anticancer agent among the 17 podophyllotoxin derivatives, showed a proliferative inhibition effect via inhibiting tubulin polymerization.

scholarly journals Novel colchicine conjugate with unusual effect on the microtubules of cancer cells

2020 ◽  
Vol 92 (8) ◽  
pp. 1217-1226
Author(s):  
Olga N. Zefirova ◽  
Evgenia V. Nurieva ◽  
Birgit Wobith ◽  
Svetlana Schulz ◽  
Nikolay A. Zefirov ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Anticancer Agent ◽  
Research Data ◽  
Tubulin Polymerization ◽  
Structure Activity ◽  
Associated Proteins ◽  
Colchicine Derivative ◽  
Colchicine Derivatives

AbstractColchicine derivative bearing substituted bispidine moiety, namely N-{7-(3,7-Di-(tert-butoxycarbonyl)-1,5-dimethyl-3,7-diazabicyclo[3.3.1]nonan-9-yl)-oxy-7-oxoheptanoyl}-N-deacetylcolchicine, was synthesized and tested for its effect on the net of microtubules (MT) in lung cancer cells A549. The compound induced not only MT depolymerization but stimulated the formation of small tubulin aggregates and long tubulin fibrils localized mainly around nuclei. The assemblies were morphologically different from tubulin clusters induced by structurally related anticancer agent tubuloclustin. The biotests data demonstrate that the depolymerization takes place for both pure tubulin and tubulin in cellulo, while fibrils are formed only in the cells. The research data of structure–activity relationship for several similar colchicine derivatives synthesized in the work give evidence for the proposition that the initial conjugate may interact not only with tubulin and MT in the cells, but also with MT-associated proteins, involved in the process of tubulin polymerization. The ability to affect simultaneously MAP – tubulin interactions opens attractive prospects in the design of novel anticancer agents.

Arsenic Trioxide Exerts Anti-lung Cancer Activity by Inhibiting Angiogenesis

2014 ◽  
Vol 14 (6) ◽  
pp. 557-566 ◽  
Author(s):  
Meng-Hang Yang ◽  
Yuan-Sheng Zang ◽  
Hai Huang ◽  
Kun Chen ◽  
Bing Li ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Arsenic Trioxide ◽  
Cancer Activity

scholarly journals Simple Thalidomide Analogs in Melanoma: Synthesis and Biological Activity

2021 ◽  
Vol 11 (13) ◽  
pp. 5823
Author(s):  
Alexia Barbarossa ◽  
Alessia Catalano ◽  
Jessica Ceramella ◽  
Alessia Carocci ◽  
Domenico Iacopetta ◽  
...  
Keyword(s):  
Anticancer Agent ◽  
Ring System ◽  
In Vitro Assays ◽  
Tubulin Polymerization ◽  
Cytotoxic Effects ◽  
Ongoing Research ◽  
Drug Candidates ◽  
Small Series ◽  
Clinical Interest

Thalidomide is an old well-known drug that is still of clinical interest, despite its teratogenic activities, due to its antiangiogenic and immunomodulatory properties. Therefore, efforts to design safer and effective thalidomide analogs are continually ongoing. Research studies on thalidomide analogs have revealed that the phthalimide ring system is an essential pharmacophoric fragment; thus, many phthalimidic compounds have been synthesized and evaluated as anticancer drug candidates. In this study, a panel of selected in vitro assays, performed on a small series of phthalimide derivatives, allowed us to characterize compound 2k as a good anticancer agent, acting on A2058 melanoma cell line, which causes cell death by apoptosis due to its capability to inhibit tubulin polymerization. The obtained data were confirmed by in silico assays. No cytotoxic effects on normal cells have been detected for this compound that proves to be a valid candidate for further investigations to achieve new insights on possible mechanism of action of this class of compounds as anticancer drugs.

scholarly journals The red wine component ellagic acid induces autophagy and exhibits anti-lung cancer activity in vitro and in vivo

2018 ◽  
Vol 23 (1) ◽  
pp. 143-154 ◽  
Author(s):  
Jing Duan ◽  
Ji-Cheng Zhan ◽  
Gui-Zhen Wang ◽  
Xin-Chun Zhao ◽  
Wei-Dong Huang ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Ellagic Acid ◽  
Red Wine ◽  
Cancer Activity

scholarly journals A novel anticancer agent SNG1153 inhibits growth of lung cancer stem/progenitor cells

Oncotarget ◽  
2016 ◽  
Vol 7 (29) ◽  
pp. 45158-45170 ◽  
Author(s):  
Shiyang Liu ◽  
Yuming Guo ◽  
Jing Wang ◽  
Hai Zhu ◽  
Yuqing Han ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Progenitor Cells ◽  
Anticancer Agent

C5-curcuminoid-dithiocarbamate based molecular hybrids: synthesis and anti-inflammatory and anti-cancer activity evaluation

RSC Advances ◽  
2014 ◽  
Vol 4 (54) ◽  
pp. 28756-28764 ◽  
Author(s):  
Amit Anthwal ◽  
Kundan Singh ◽  
M. S. M. Rawat ◽  
Amit K. Tyagi ◽  
Bharat B. Aggarwal ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Activity Evaluation ◽  
Anti Cancer ◽  
Molecular Hybrids ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Cancer Activity ◽  
Proliferation Potential

The C5-curcumin-dithiocarbamate analogues were synthesized in search of new molecules with anti-proliferation potential against cancer cells. These new compounds demonstrated higher anti-proliferation and anti-inflammatory activity against cancer cell lines in comparison to curcumin.

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