scholarly journals Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin

MedChemComm ◽  
2015 ◽  
Vol 6 (5) ◽  
pp. 788-794 ◽  
Author(s):  
Nikhil R. Madadi ◽  
Hongliang Zong ◽  
Amit Ketkar ◽  
Chen Zheng ◽  
Narsimha R. Penthala ◽  
...  

Novel resveratrol analogues have been synthesized and evaluated for their anticancer activities against a panel of 60 human cancer cell lines.

2019 ◽  
Vol 46 (2) ◽  
pp. 2059-2066 ◽  
Author(s):  
Asghar Arshi ◽  
Sayed Mostafa Hosseini ◽  
Fataneh Saleh Khaje Hosseini ◽  
Zahra Yousefnejad Amiri ◽  
Fatemeh Sadat Hosseini ◽  
...  

2021 ◽  
Author(s):  
Cheng-Ting Zi ◽  
Bo-Ya Shi ◽  
Ze-Hao Wang ◽  
Ning Zhang ◽  
Yin-Rong Xie ◽  
...  

Abstract Novel glucosylated (-)-epigallocatechin-3-gallate derivatives 10 – 13 having the EGCG analogues conjugated to the D-glucosyl azide were synthesized by carrying out the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction, and were evaluated for their cytotoxicities against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using MTT assays. Compounds 10 and 11 showed the highest levels of cytotoxicity against the HL-60 cells with IC50 values of 4.57 μM and 3.78 μM, respectively, and showed moderate selectivity towards cancer cell lines. Compound 11 was also shown to induce apoptosis in HL-60 cells. Most notably, inclusion of the perbutyrylated glucose residue in an EGCG derivative was concluded to lead to increased anticancer activity.


2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Sergey A. Dyshlovoy ◽  
Sergey N. Fedorov ◽  
Larisa K. Shubina ◽  
Alexandra S. Kuzmich ◽  
Carsten Bokemeyer ◽  
...  

Aaptamine (8,9-dimethoxy-1H-benzo[de][1,6]naphthyridine) is a marine natural compound possessing antioxidative, antimicrobial, antifungal, and antiretroviral activity. Earlier, we have found that aaptamine and its derivatives demonstrate equal anticancer effects against the human germ cell cancer cell lines NT2 and NT2-R and cause some changes in the proteome of these cells. In order to explore further the mechanism of action of aaptamine and its derivatives, we studied the effects of aaptamine (1), demethyl(oxy)aaptamine (2), and isoaaptamine (3) on human cancer cell lines and on AP-1-, NF-κB-, and p53-dependent transcriptional activity in murine JB6 Cl41 cells. We showed that compounds1–3demonstrate anticancer activity in THP-1, HeLa, SNU-C4, SK-MEL-28, and MDA-MB-231 human cancer cell lines. Additionally, all compounds were found to prevent EGF-induced neoplastic transformation of murine JB6 Cl41 cells. Nuclear factors AP-1, NF-κB, and p53 are involved in the cellular response to high and nontoxic concentrations of aaptamine alkaloids1–3. Furthermore, inhibition of EGF-induced JB6 cell transformation, which is exerted by the compounds1–3at low nontoxic concentrations of 0.7–2.1 μM, cannot be explained by activation of AP-1 and NF-κB.


2020 ◽  
Author(s):  
Reine Hanna ◽  
Reem Daouk ◽  
Farah Ballout ◽  
Sarra El-Soussie ◽  
Jad Abdallah ◽  
...  

2021 ◽  
Vol 18 ◽  
Author(s):  
Tran Khac Vu ◽  
Bach Xuan Nguyen ◽  
Linh Nguyen Pham Duy ◽  
Thuc Bao Nguyen Truong ◽  
Anh Tuan Phung ◽  
...  

Background: In this study, two novel hybrid series of artemisinin and quinazolinones were synthesized and evaluated in vitro cytotoxicity against two human cancer cell lines, including SKLu-1 (lung cancer), MCF- 7 (breast cancer). The bio-assay results indicated that most of the target compounds exhibited cytotoxic activities against both human cancer cell lines tested, and seemed to be more cytotoxic toward the breast (MCF-7) cancer cells than lung (SKLu-1) cancer cells. Among the synthesized artemisinin hybrids, the compound 13d containing a quinazolinone conjugated system exhibited the most potent cytotoxicity against the SKLu-1 and MCF-7 cell lines with IC50 values of 1.62 and 0.77 µM, respectively. Objective: This study aims at developing novel hybrids of artemisinin and quinazolinones as anti-cancer agents. Method: A series of novel hybrids were designed, synthesized and evaluated for cytotoxicity against two human cancer cell lines, including SKLu-1 and MCF-7 using SRB method. Results : All thirteen hybrids of artemisinin with quinazolinone exhibited cytotoxic activity against two tested cancer cell lines, in which the compound 13d exhibited the most potent cytotoxicity against the SKLu-1 and MCF-7 cell lines with IC50 values of 1.62 and 0.77 µM, respectively. Conclusion: The research results suggest that some compounds could be considered as leads for future design of hybrids and have the potential for further studies in the field of anti-cancer agent development.


2018 ◽  
Vol 18 (5) ◽  
pp. 765-765
Author(s):  
Dhanyalayam D ◽  
Palma G ◽  
Cappello AR ◽  
Mariconda A ◽  
Sinicropi MS ◽  
...  

Due to an oversight one of the author’s name was published wrong in the article entitled “Phosphonium Salt Displays Cytotoxic Effects Against Human Cancer Cell Lines” in “Anti-Cancer Agents in Medicinal Chemistry, 2015, Vol. 17, No. 13. pp. 1796.” <p> The correct names of all authors are given below: <p> Dhanyalayam D, Palma G, Cappello AR, Mariconda A, Sinicropi MS, Giordano F, Del Vecchio V, Ramunno A, Arra C, Longo P, Saturnino C.


MedChemComm ◽  
2019 ◽  
Vol 10 (8) ◽  
pp. 1488-1498 ◽  
Author(s):  
Radmila R. Sharipova ◽  
Mayya G. Belenok ◽  
Bulat F. Garifullin ◽  
Anastasiya S. Sapunova ◽  
Alexandra D. Voloshina ◽  
...  

A series of glycosides and glycoconjugates of diterpenoid isosteviol with various monosaccharide residues were synthesized. Most of them showed moderate to significant cytotoxicity against human cancer cell lines M-HeLa and MCF-7.


2015 ◽  
Vol 29 (S1) ◽  
Author(s):  
Tawna Whited ◽  
Bryce Adams ◽  
Christopher Stang ◽  
Thomas Pierson ◽  
Rahul Khupse ◽  
...  

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