Characterization of novel heterocyclic compounds based on 4-aryl-4H-chromene scaffold as anticancer agents: Design, synthesis, antiprofilerative activity against resistant cancer cells, dual β-tubulin/c-Src inhibition, cell cycle arrest and apoptosis induction

2021 ◽  
pp. 105591
Author(s):  
Eman K.A. Abdelall ◽  
Heba A. H. Elshemy ◽  
Madlen B. Labib ◽  
Fatma E. A. Mohamed
2017 ◽  
Vol 85 ◽  
pp. 425-433 ◽  
Author(s):  
Luis Felipe Buso Bortolotto ◽  
Flávia Regina Barbosa ◽  
Gabriel Silva ◽  
Tamires Aparecida Bitencourt ◽  
Rene Oliveira Beleboni ◽  
...  

Oncotarget ◽  
2016 ◽  
Vol 7 (17) ◽  
pp. 24027-24049 ◽  
Author(s):  
Cristina Florean ◽  
Michael Schnekenburger ◽  
Jin-Young Lee ◽  
Kyung Rok Kim ◽  
Aloran Mazumder ◽  
...  

2021 ◽  
Vol 14 (11) ◽  
pp. 1108
Author(s):  
Hung-Tse Huang ◽  
Chia-Ching Liaw ◽  
Yu-Chi Lin ◽  
Geng-You Liao ◽  
Chih-Hua Chao ◽  
...  

Mesona procumbens is a popular material used in foods and herbal medicines in Asia for clearing heat and resolving toxins. However, phytochemical research on this plant is very rare. In this study, eleven new diterpenoids, mesonols A-K (1–11), comprising seven ent-kauranes, three ent-atisanes, and one sarcopetalane, were isolated from its methanolic extract. Structural elucidation of compounds 1–11 was performed by spectroscopic methods, especially 2D NMR, HRESIMS, and X-ray crystallographic analysis. All isolates were assessed for their antiproliferative activity, and compounds 1-4 showed potential antiproliferative activities against A549, Hep-3B, PC-3, HT29, and U937 cancer cells, with IC50 values ranging from 1.97 to 19.86 µM. The most active compounds, 1 and 2, were selected for further investigation of their effects on cell cycle progression, apoptosis, and ROS generation in U937 human leukemia cancer cells. Interestingly, it was found that compounds 1 and 2 induced antiproliferative effects in U937 cells through different mechanisms. Compound 1 caused cell cycle arrest at the G2/M phase and subsequent cell death in a dose- and time-dependent manner. However, 2-mediated antiproliferation of U937 cells triggered ROS-mediated mitochondrial-dependent apoptosis. These results provide insight into the molecular mechanism involved in the antiproliferative activities of compounds 1 and 2 in U937 cells. Altogether, the study showed that new diterpenoid compounds 1 and 2 from M. procumbens are potent and promising anticancer agents.


RSC Advances ◽  
2015 ◽  
Vol 5 (40) ◽  
pp. 31759-31767 ◽  
Author(s):  
Shahla Karim Baloch ◽  
Lin Ma ◽  
Xue-Liang Wang ◽  
Jing Shi ◽  
Yu Zhu ◽  
...  

Novel shikonin derivatives were synthesised and probed as anticancer agents. Compound 40 showed the best anticancer activity with an IC50 of 1.26 μM, could induce apoptosis and cause cell cycle arrest at the G2/M phase via the P21 p-CDC2 (Tyr15) pathway independent of P53.


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