Synthesis and molecular structure of arene ruthenium(ii) benzhydrazone complexes: impact of substitution at the chelating ligand and arene moiety on antiproliferative activity

2016 ◽  
Vol 40 (11) ◽  
pp. 9813-9823 ◽  
Author(s):  
Mohamed Kasim Mohamed Subarkhan ◽  
Rengan Ramesh ◽  
Yu Liu
Keyword(s):  
Molecular Structure ◽  
Cancer Cells ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Arene Complexes ◽  
Anticancer Activities ◽  
Human Cancer Cells ◽  
Chelating Ligand

A series of ruthenium(ii) arene complexes have been synthesized and evaluated for their in vitro anticancer activities. The complexes exhibit promising anticancer activities in human cancer cells.

Structural characterization of new zinc(ii) complexes with N2O2 chelating thiosemicarbazidato ligands; investigation of the relationship between their DNA interaction and in vitro antiproliferative activity towards human cancer cells

2020 ◽  
Vol 44 (22) ◽  
pp. 9313-9320
Author(s):  
Büşra Kaya ◽  
Zehra Kübra Yılmaz ◽  
Onur Şahin ◽  
Belma Aslim ◽  
Bahri Ülküseven
Keyword(s):  
Cancer Cells ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Dna Interaction ◽  
Antiproliferative Agents ◽  
Human Cancer Cells ◽  
Dna Targeting ◽  
The Relationship

New candidates to become DNA-targeting antiproliferative agents: Zinc(ii) complexes bearing N2O2-thiosemicarbazidato ligands.

Ruthenium(ii) arene complexes containing benzhydrazone ligands: synthesis, structure and antiproliferative activity

2016 ◽  
Vol 3 (10) ◽  
pp. 1245-1255 ◽  
Author(s):  
Mohamed Kasim Mohamed Subarkhan ◽  
Rengan Ramesh
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Arene Complexes ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells

Six new Ru(ii) arene anthracene benzhydrazone complexes have been synthesized and show excellent cytotoxicity against human cancer cell lines. The results of apoptosis assays demonstrated that complexes4and6are able to induce apoptosis in human cancer cells.

scholarly journals A New Smoothened Antagonist Bearing the Purine Scaffold Shows Antitumour Activity In Vitro and In Vivo

2021 ◽  
Vol 22 (16) ◽  
pp. 8372
Author(s):  
Ana María Zárate ◽  
Christian Espinosa-Bustos ◽  
Simón Guerrero ◽  
Angélica Fierro ◽  
Felipe Oyarzún-Ampuero ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Antitumour Activity ◽  
Anticancer Compounds ◽  
Human Cancer Cells ◽  
Cycle Arrest ◽  
Apoptosis Inducer ◽  
Purine Ring

The Smoothened (SMO) receptor is the most druggable target in the Hedgehog (HH) pathway for anticancer compounds. However, SMO antagonists such as vismodegib rapidly develop drug resistance. In this study, new SMO antagonists having the versatile purine ring as a scaffold were designed, synthesised, and biologically tested to provide an insight to their mechanism of action. Compound 4s was the most active and the best inhibitor of cell growth and selectively cytotoxic to cancer cells. 4s induced cell cycle arrest, apoptosis, a reduction in colony formation and downregulation of PTCH and GLI1 expression. BODIPY-cyclopamine displacement assays confirmed 4s is a SMO antagonist. In vivo, 4s strongly inhibited tumour relapse and metastasis of melanoma cells in mice. In vitro, 4s was more efficient than vismodegib to induce apoptosis in human cancer cells and that might be attributed to its dual ability to function as a SMO antagonist and apoptosis inducer.

Rhodium(i) N-heterocyclic carbene complexes: synthesis and cytotoxic properties

2021 ◽  
Vol 45 (11) ◽  
pp. 5176-5183
Author(s):  
Ichraf Slimani ◽  
Serap Şahin-Bölükbaşı ◽  
Mustafa Ulu ◽  
Enes Evren ◽  
Nevin Gürbüz ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Mtt Assay ◽  
Incubation Time ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Carbene Complexes ◽  
Human Cancer Cells ◽  
Benzimidazolium Salts ◽  
Ht 29

A series of benzimidazolium salts and their [RhCl(NHC)(COD)] complexes were synthesized. All compounds were screened for in vitro cytotoxic activities against a panel of human cancer cells (HT-29 colon, Ishikawa endometrial, U-87 glioblastoma) using the MTT assay for 48 h incubation time.

scholarly journals Antiproliferative activity and induction of apoptosis by Annona muricata (Annonaceae) extract on human cancer cells

2014 ◽  
Vol 14 (1) ◽  
Author(s):  
Constant Anatole Pieme ◽  
Santosh Guru Kumar ◽  
Mireille Sylviane Dongmo ◽  
Bruno Moukette Moukette ◽  
Fabrice Fekam Boyoum ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Annona Muricata ◽  
Human Cancer Cells ◽  
Induction Of Apoptosis

Multicomponent 5-fluorouracil loaded PAMAM stabilized-silver nanocomposites synergistically induce apoptosis in human cancer cells

2015 ◽  
Vol 3 (3) ◽  
pp. 457-468 ◽  
Author(s):  
Ishita Matai ◽  
Abhay Sachdev ◽  
P. Gopinath
Keyword(s):  
Cancer Therapy ◽  
Cancer Cells ◽  
Therapeutic Agent ◽  
Human Cancer ◽  
Pamam Dendrimer ◽  
Human Cancer Cells ◽  
Silver Nanocomposites

Herein, we report the development of a poly(amidoamine) (PAMAM) dendrimer based multicomponent therapeutic agent forin vitrocancer therapy applications.

scholarly journals Effect of Calomelanone, a Dihydrochalcone Analogue, on Human Cancer Apoptosis/Regulated Cell Death in an In Vitro Model

2020 ◽  
Vol 2020 ◽  
pp. 1-16
Author(s):  
Wasitta Rachakhom ◽  
Ratana Banjerdpongchai
Keyword(s):  
Cell Death ◽  
Cancer Cells ◽  
Hepg2 Cells ◽  
Cytotoxic Effect ◽  
Human Cancer ◽  
Autophagic Flux ◽  
Dependent Manner ◽  
Anticancer Activities ◽  
Human Cancer Cells ◽  
Regulated Cell Death

Calomelanone, 2 ′ ,6 ′ -dihydroxy-4,4 ′ -dimethoxydihydrochalcone, possesses anticancer activities. This study was conducted to investigate the cytotoxic effect of calomelanone, a dihydrochalcone analogue, on human cancer cells and its associated mechanisms. The cytotoxic effect of calomelanone was measured by MTT assay. Annexin V-FITC/propidium iodide and DiOC6 staining that employed flow cytometry were used to determine the mode of cell death and reduction of mitochondrial transmembrane potential (MTP), respectively. Caspase activities were measured using specific substrates and colorimetric analysis. The expression levels of Bcl-2 family proteins were determined by immunoblotting. Reactive oxygen species were also measured using 2 ′ ,7 ′ -dihydrodichlorofluorescein diacetate and dihydroethidium (fluorescence dyes). Calomelanone was found to be toxic towards various human cancer cells, including acute promyelocytic HL-60 and monocytic leukemic U937 cells, in a dose-dependent manner at 24 h and human hepatocellular HepG2 cells at 48 h. However, the proliferation of HepG2 cells increased at 24 h. Calomelanone was found to induce apoptosis in HL-60 and U937 at 24 h and HepG2 apoptosis at 48 h via the intrinsic pathway by inducing MTP disruption. This compound also induced caspase-3, caspase-8, and caspase-9 activities. Calomelanone upregulated proapoptotic Bax and Bak and downregulated antiapoptotic Bcl-xL proteins in HepG2 cells. Moreover, signaling was also associated with oxidative stress in HepG2 cells. Calomelanone induced autophagy at 24 h of treatment, which was evidenced by staining with monodansylcadaverine (MDC) to represent autophagic flux. This was associated with a decrease of Akt (survival pathway) and an upregulation of Atg5 (the marker of autophagy). Thus, calomelanone induced apoptosis/regulated cell death in HL-60, U937, and HepG2 cells. However, it also induced autophagy in HepG2 depending on duration, dose, and type of cells. Thus, calomelanone could be used as a potential anticancer agent for cancer treatment. Nevertheless, acute and chronic toxicity should be further investigated in animals before conducting investigations in human patients.

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