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.

Flavonoid-Based Cancer Therapy: An Updated Review

2020 ◽  
Vol 20 (12) ◽  
pp. 1398-1414 ◽  
Author(s):  
Elham Hosseinzadeh ◽  
Ali Hassanzadeh ◽  
Faroogh Marofi ◽  
Mohammad Reza Alivand ◽  
Saeed Solali
Keyword(s):  
Cancer Therapy ◽  
Cancer Cells ◽  
Human Cancer ◽  
Human Cancer Cells ◽  
Anti Cancer ◽  
Phytochemical Compounds ◽  
Proliferation And Metastasis ◽  
The Relationship

: As cancers are one of the most important causes of human morbidity and mortality worldwide, researchers try to discover novel compounds and therapeutic approaches to decrease survival of cancer cells, angiogenesis, proliferation and metastasis. In the last decade, use of special phytochemical compounds and flavonoids was reported to be an interesting and hopeful tactic in the field of cancer therapy. Flavonoids are natural polyphenols found in plant, fruits, vegetables, teas and medicinal herbs. Based on reports, over 10,000 flavonoids have been detected and categorized into several subclasses, including flavonols, anthocyanins, flavanones, flavones, isoflavones and chalcones. It seems that the anticancer effect of flavonoids is mainly due to their antioxidant and anti inflammatory activities and their potential to modulate molecular targets and signaling pathways involved in cell survival, proliferation, differentiation, migration, angiogenesis and hormone activities. The main aim of this review is to evaluate the relationship between flavonoids consumption and cancer risk, and discuss the anti-cancer effects of these natural compounds in human cancer cells. Hence, we tried to collect and revise important recent in vivo and in vitro researches about the most effective flavonoids and their main mechanisms of action in various types of cancer cells.

scholarly journals In Vitro Characterization of an Anti-HER2 Affibody-Monomethyl Auristatin E Conjugate in HER2-Positive Breast Cancer Cells

2021 ◽  
Vol 7 (1) ◽  
pp. 3
Author(s):  
Isabella Damiani ◽  
Silvia Castiglioni ◽  
Valentina Rusconi ◽  
Clara Rossi ◽  
Alberto Corsini ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Binding Affinities ◽  
Her2 Positive ◽  
Human Cancer Cells ◽  
Protein Levels ◽  
Drug Conjugates ◽  
In Vitro Characterization

Antibody-drug conjugates (ADCs) are used in anticancer therapy with some limitations due to their molecular properties. An alternative to monoclonal antibodies is the affibody, composed of 58 amino acids, with lower binding affinities, small size, and rapid blood clearance and tissue distribution. We investigate the in vitro efficacy of a novel anti-HER2 ZHER2:2891 affibody conjugated to a cytotoxic drug auristatin E (MMAE) in HER2-positive human cancer cells. An adenocarcinoma cell line SK-BR-3, expressing high levels of HER2, and mammary gland adenocarcinoma MDA-MB-231, expressing basal levels of HER2, were treated with ZHER2:2891DCS-MMAE and trastuzumab (as a reference compound). ZHER2:2891DCS-MMAE induced a significant time-dependent toxic effect in SK-BR-3 cells. A 30% reduction in cell viability was found after 10 min exposure at 7 nM with an IC50 of 80.2 nM. On the contrary, MDA-MB-231 cells were not affected by the affibody complex. The HER2-specific cytotoxic effect of the ZHER2:2891DCS-MMAE has also been confirmed by measuring apoptosis by flow cytometry. In SK-BR-3 cells, the increasing concentrations of the conjugated affibody induced cell death after 10 min of treatment with the strongest effect observed after 48 h. Moreover, treatment with ZHER2:2891DCS-MMAE reduced (up to 50%) HER2 expression at both mRNA and protein levels in SK-BR-3 cells after 24 h of treatment. In conclusion, the cytotoxic conjugate based on the anti-HER2 affibody and MMAE efficiently interacts with HER2 over-expressing cancer cells, allowing the selective and specific delivery of the cytotoxic payload. The basal HER2 expressing cells are not the most affected probably due to a lower uptake of the drug conjugate. This confirms that affibodies may be used to target HER2 overexpressing cells while sparing normal cells.

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.

Characterization of novel Checkpoint kinase 1 inhibitors by in vitro assays and in human cancer cells treated with topoisomerase inhibitors

Life Sciences ◽  
2011 ◽  
Vol 89 (7-8) ◽  
pp. 259-268 ◽  
Author(s):  
Gilles Ferry ◽  
Aurélie Studeny ◽  
Céline Bossard ◽  
Philip M. Kubara ◽  
Denis Zeyer ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
In Vitro Assays ◽  
Topoisomerase Inhibitors ◽  
Checkpoint Kinase ◽  
Checkpoint Kinase 1 ◽  
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
Sign in / Sign up

Export Citation Format

Share Document