Novel phosphine sulphide gold(i) complexes: topoisomerase I inhibitors and antiproliferative agents

2020 ◽  
Vol 49 (23) ◽  
pp. 7852-7861
Author(s):  
Endika Martín-Encinas ◽  
Verónica Conejo-Rodríguez ◽  
Jesús A. Miguel ◽  
Jesús M. Martínez-Ilarduya ◽  
Gloria Rubiales ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Topoisomerase I ◽  
Cancer Cell Lines ◽  
Antiproliferative Agents ◽  
Topoisomerase I Inhibitors ◽  
Phosphine Sulfide

Gold(i) increases the cytotoxicity of phosphine sulfide quinolines against cancer cell lines, while heterocycles maintain the TopI inhibitory activity.

scholarly journals Modifications on the Tetrahydroquinoline Scaffold Targeting a Phenylalanine Cluster on GPER as Antiproliferative Compounds against Renal, Liver and Pancreatic Cancer Cells

2021 ◽  
Vol 14 (1) ◽  
pp. 49
Author(s):  
David Méndez-Luna ◽  
Loreley Araceli Morelos-Garnica ◽  
Juan Benjamín García-Vázquez ◽  
Martiniano Bello ◽  
Itzia Irene Padilla-Martínez ◽  
...  
Keyword(s):  
Binding Site ◽  
Cell Lines ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
In Silico ◽  
Cancer Cell Lines ◽  
Pancreatic Cancer Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
New Compounds

The implementation of chemo- and bioinformatics tools is a crucial step in the design of structure-based drugs, enabling the identification of more specific and effective molecules against cancer without side effects. In this study, three new compounds were designed and synthesized with suitable absorption, distribution, metabolism, excretion and toxicity (ADME-tox) properties and high affinity for the G protein-coupled estrogen receptor (GPER) binding site by in silico methods, which correlated with the growth inhibitory activity tested in a cluster of cancer cell lines. Docking and molecular dynamics (MD) simulations accompanied by a molecular mechanics/generalized Born surface area (MMGBSA) approach yielded the binding modes and energetic features of the proposed compounds on GPER. These in silico studies showed that the compounds reached the GPER binding site, establishing interactions with a phenylalanine cluster (F206, F208 and F278) required for GPER molecular recognition of its agonist and antagonist ligands. Finally, a 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyltetrazolium bromide (MTT) assay showed growth inhibitory activity of compounds 4, 5 and 7 in three different cancer cell lines—MIA Paca-2, RCC4-VA and Hep G2—at micromolar concentrations. These new molecules with specific chemical modifications of the GPER pharmacophore open up the possibility of generating new compounds capable of reaching the GPER binding site with potential growth inhibitory activities against nonconventional GPER cell models.

scholarly journals Design, Synthesis and Biological Evaluation of a New Series of 1-Aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea Derivatives as Antiproliferative Agents

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2108 ◽  
Author(s):  
Chuanming Zhang ◽  
Xiaoyu Tan ◽  
Jian Feng ◽  
Ning Ding ◽  
Yongpeng Li ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
A549 Cells ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Urea Derivatives ◽  
Antiproliferative Agents

To discover new antiproliferative agents with high efficacy and selectivity, a new series of 1-aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea derivatives (7a–7t) were designed, synthesized and evaluated for their antiproliferative activity against A549, HCT-116 and PC-3 cancer cell lines in vitro. Most of the target compounds demonstrated significant antiproliferative effects on all the selective cancer cell lines. Among them, the target compound, 1-[4-chloro-3-(trifluoromethyl)phenyl]-3-{4-{{[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methyl}thio}phenyl}urea (7i) was identified to be the most active one against three cell lines, which was more potent than the positive control with an IC50 value of 1.53 ± 0.46, 1.11 ± 0.34 and 1.98 ± 1.27 μM, respectively. Further cellular mechanism studies confirmed that compound 7i could induce the apoptosis of A549 cells in a concentration-dependent manner and elucidated compound 7i arrests cell cycle at G1 phase by flow cytometry analysis. Herein, the studies suggested that the 1-aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea skeleton might be regarded as new chemotypes for designing effective antiproliferative agents.

scholarly journals Synthesis and Antiproliferative activity in vitro of Amidino Substituted 2-phenylbenzazoles

2019 ◽  
Vol 92 (2) ◽  
pp. 181-189 ◽  
Author(s):  
Livio Racané ◽  
Kristina Butković ◽  
Irena Martin-Kleiner ◽  
Marijeta Kralj ◽  
Grace Karminski-Zamola ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Cancer Cell Lines ◽  
Benzimidazole Derivatives ◽  
Antiproliferative Agents ◽  
Benzothiazole Derivatives

Within this work we describe the synthesis of versatile substituted 2-phenyl benzothiazole 3–10 and 2-phenylbenzimidazole 12–19 derivatives bearing amidino groups. Furthermore, the synthesized compounds were explored for their antiproliferative activity in vitro on three cancer cell lines. Tested compounds showed moderate to strong antiproliferative activity. Furthermore, the type of the attached amidino group on benzazole nuclei has the significant impact on the antiproliferative activity only within benzimidazole derivatives with 2-imidazolinyl substituted derivatives being more active in comparison to amidino substituted analogues. All obtained results revealed that this type of benzothiazole derivatives have a great potential for further optimization and development of more efficient potential antiproliferative agents.

scholarly journals Proteomic Analysis of Nuclei Isolated from Cancer Cell Lines Treated with Indenoisoquinoline NSC 724998, a Novel Topoisomerase I Inhibitor

2010 ◽  
Vol 9 (8) ◽  
pp. 4016-4027 ◽  
Author(s):  
Bingnan Han ◽  
Luke H. Stockwin ◽  
Chad Hancock ◽  
Sherry X. Yu ◽  
Melinda G. Hollingshead ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Proteomic Analysis ◽  
Topoisomerase I ◽  
Cancer Cell Lines ◽  
Topoisomerase I Inhibitor

Histone Deacetylase Inhibitory Activity of Peanut Testa Extracts against Human Cancer Cell Lines

2015 ◽  
Vol 39 (3) ◽  
pp. 263-273 ◽  
Author(s):  
Somprasong Khaopha ◽  
Sanun Jogloy ◽  
Aran Patanothai ◽  
Thanaset Senawong
Keyword(s):  
Histone Deacetylase ◽  
Cell Lines ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines
Sign in / Sign up

Export Citation Format

Share Document