The water soluble peripherally tetra-substituted zinc(ii), manganese(iii) and copper(ii) phthalocyanines as new potential anticancer agents

2016 ◽  
Vol 45 (36) ◽  
pp. 14301-14310 ◽  
Author(s):  
Burak Barut ◽  
Ayşenur Sofuoğlu ◽  
Zekeriya Biyiklioglu ◽  
Arzu Özel
Keyword(s):  
Anticancer Agents ◽  
Plasmid Dna ◽  
Water Soluble ◽  
Ethoxy Group ◽  
Pbr322 Plasmid ◽  
Ct Dna

In this study, [2-(2-morpholin-4-ylethoxy)ethoxy] group substituted zinc(ii), manganese(iii) and copper(ii) phthalocyanines 2–4 and their water soluble derivatives 2a, 3a and 4a were synthesized and the interactions of compounds 2a, 3a and 4a with CT-DNA and supercoiled pBR322 plasmid DNA were investigated.

Study of New Ferrocene Incorporated N,N′-Disubstituted Thioureas as Potential Antitumour Agents

2013 ◽  
Vol 66 (11) ◽  
pp. 1352 ◽  
Author(s):  
Bhajan Lal ◽  
Amin Badshah ◽  
Ataf Ali Altaf ◽  
Muhammad Nawaz Tahir ◽  
Shafiq Ullah ◽  
...  
Keyword(s):  
Plasmid Dna ◽  
Electrostatic Interactions ◽  
Antitumour Activity ◽  
Conformational Stability ◽  
13C Nmr Spectroscopy ◽  
Ovarian Tumour ◽  
Structural Characterisation ◽  
Antitumour Agents ◽  
Pbr322 Plasmid ◽  
Ct Dna

In this paper, we report the synthesis, structural characterisation, cytotoxicity against human ovarian tumour models (A2780, A2780cisR, and A2780ZD0473R), nature of interaction with calf-thymus (CT)-DNA and pBR322 plasmid DNA of new ferrocene based N,N′-disubstituted thioureas (3a–d). The compounds, characterized based on elemental analysis, FT-IR and multinuclear (1H and 13C) NMR spectroscopy, and single crystal X-ray diffractometry, were found to have significant antitumour activity although much less than cisplatin. Crystallographic data reveals the existance of secondary interactions for compound 3c in terms of intermolecular hydrogen bonding of type NH⋯O, NH⋯S and secondary non-covalent interactions (π⋯H). When pBR322 plasmid DNA was interacted with increasing concentrations of compounds, 3a and 3b but not 3c were found to partially prevent BamH1 digestion of the DNA. The negative shift in peak potential in voltammetric measurements indicates that all the compounds undergo electrostatic interactions with the negatively charged phosphate DNA backbone. The large negative value of the binding energy indicates the spontaneity of reaction between the compounds and CT-DNA and the conformational stability of adducts formed.

scholarly journals Studies of the Antiproliferative Activity of Ruthenium (II) Cyclopentadienyl-Derived Complexes with Nitrogen Coordinated Ligands

2010 ◽  
Vol 2010 ◽  
pp. 1-11 ◽  
Author(s):  
Virtudes Moreno ◽  
Julia Lorenzo ◽  
Francesc X. Aviles ◽  
M. Helena Garcia ◽  
João P. Ribeiro ◽  
...  
Keyword(s):  
Plasmid Dna ◽  
Antitumor Agents ◽  
Tertiary Structure ◽  
Base Pairs ◽  
Force Microscopy ◽  
Atomic Force ◽  
Dna Base ◽  
Dna Base Pairs ◽  
Pbr322 Plasmid ◽  
Ct Dna

Four cationic ruthenium(II) complexes with the formula[Ru(η5-C5H5)(PPh3)2]+, withL=5-phenyl-1H-tetrazole (TzH)1, imidazole (ImH)2, benzo[1,2-b;4,3-b′] dithio-phen-2-carbonitrile (Bzt)3, and [5-(2-thiophen-2-yl)-vinyl]-thiophene-2-carbonitrile] (Tvt)4were prepared and characterized in view to evaluate their potentialities as antitumor agents. Studies by Circular Dichroism indicated changes in the secondary structure of ct-DNA. Changes in the tertiary structure of pBR322 plasmid DNA were also observed in gel electrophoresis experiment and the images obtained by atomic force microscopy (AFM) suggest strong interaction with pBR322 plasmid DNA; the observed decreasing of the viscosity with time indicates that the complexes do not intercalate between DNA base pairs. Compounds1,2, and3showed much higher cytotoxicity than the cisplatin against human leukaemia cancer cells (HL-60 cells).

scholarly journals Activity of Indenoisoquinolines against African Trypanosomes

2008 ◽  
Vol 53 (1) ◽  
pp. 123-128 ◽  
Author(s):  
Rahul P. Bakshi ◽  
Dongpei Sang ◽  
Andrew Morrell ◽  
Mark Cushman ◽  
Theresa A. Shapiro
Keyword(s):  
Anticancer Agents ◽  
Mammalian Cells ◽  
Sleeping Sickness ◽  
Water Soluble ◽  
African Trypanosomes ◽  
In Vivo Experiments ◽  
Topoisomerase Ib ◽  
Topoisomerase Poisons

ABSTRACT African trypanosomiasis (sleeping sickness), caused by protozoan Trypanosoma brucei species, is a debilitating disease that is lethal if untreated. Available drugs are antiquated, toxic, and compromised by emerging resistance. The indenoisoquinolines are a class of noncamptothecin topoisomerase IB poisons that are under development as anticancer agents. We tested a variety of indenoisoquinolines for their ability to kill T. brucei. Indenoisoquinolines proved trypanocidal at submicromolar concentrations in vitro. Structure-activity analysis yielded motifs that enhanced potency, including alkylamino substitutions on N-6, methoxy groups on C-2 and C-3, and a methylenedioxy bridge between C-8 and C-9. Detailed analysis of eight water-soluble indenoisoquinolines demonstrated that in trypanosomes the compounds inhibited DNA synthesis and acted as topoisomerase poisons. Testing these compounds on L1210 mouse leukemia cells revealed that all eight were more effective against trypanosomes than against mammalian cells. In preliminary in vivo experiments one compound delayed parasitemia and extended survival in mice subjected to a lethal trypanosome challenge. The indenoisoquinolines provide a promising lead for the development of drugs against sleeping sickness.

Advancements in the Use of Platinum Complexes as Anticancer Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Rajiv Sharma ◽  
Vikram Jeet Singh ◽  
Pooja A Chawla
Keyword(s):  
Anticancer Agents ◽  
Biomedical Applications ◽  
Clinical Importance ◽  
Platinum Complexes ◽  
Water Soluble ◽  
Platinum Compounds ◽  
Anticancer Compounds ◽  
Cellular Resistance ◽  
Anti Cancer ◽  
Target Effects

Background: The platinum (II) complexes as anticancer agents have been well explored for the development of novel analogs. Yet, none of them achieved clinical importance in oncology. At present, anticancer compounds containing platinum (II) complexes have been employed in the treatment of colorectal, lung, and genitourinary tumors. Among the platinum-based anticancer drugs, Cisplatin (cis-diamine dichloroplatinum (II), cis-[Pt(NH3)2Cl2]) is one of the most potent components of cancer chemotherapy. The nephrotoxicity, neurotoxicity and ototoxicity, and platinum compounds associated resistant cancer are some major disadvantages. Objective: With the rapidly growing interest in platinum (II) complexes in tumor chemotherapy, researchers have synthesized many new platinum analogs as anticancer agents that show better cytotoxicity, and less off-target effects with less cellular resistance. This follows the introduction of oxaliplatin, water-soluble carboplatin, multinuclear platinum and newly synthesized complexes, etc. Method: This review emphasizes recent advancements in drug design and development, the mechanism of platinum (II) complexes, their stereochemistry, current updates, and biomedical applications of platinum-based anticancer agents. Conclusion: In the last few decades, the popularity of platinum complexes as potent anti-cancer agents has risen as scientists have synthesized many new platinum complexes that exhibit better cytotoxicity coupled with less off-target effects.

scholarly journals Synthesis, DNA-binding and antiproliferative activity of N-(Nitrogen heterocyclic) norcantharidin acylamide acid

2009 ◽  
Vol 7 (3) ◽  
pp. 569-575 ◽  
Author(s):  
Wen-Zhong Zhu ◽  
Rui-Ding Hu ◽  
Qiu-Yue Lin ◽  
Xiao-Xia Wang ◽  
Xiao-Liang Zheng
Keyword(s):  
Dna Binding ◽  
Cell Line ◽  
Elemental Analysis ◽  
Antiproliferative Activity ◽  
Plasmid Dna ◽  
H Nmr ◽  
Smmc7721 Cell ◽  
Calf Thymus ◽  
Binding Experiment ◽  
Pbr322 Plasmid

AbstractTwo novel norcantharidin acylamide acids (HL1=N-pyrimidine norcantharidin acylamide acid, C12H13N3O4; HL2=N-pyridine norcantharidin acylamide acid, C13H14N2O4) were synthesized by a reaction of norcantharidin(NCTD) with 2-aminopyrimidine and 2-aminopyridine, respectively. Their structures were characterized by elemental analysis, IR, UV and 1 H NMR. Fluorescence titration and viscosity measurements indicated that HL1, HL2 and HL3 (HL3=N-phenyl norcantharidin acylamide acid, C14H15NO4) can bind calf thymus DNA via partial intercalation. The liner Stern-Volmer quenching constant Ksv values for HL1, HL2 and HL3 were 2.05 × 104 L mol−1, 1.15 × 104 L mol−1 and 8.30×103 L mol−1, respectively. Two compounds containing heterocycle of HL1 and HL2 have been found to cleave pBR322 plasmid DNA at physiological pH and temperature. The test of antiproliferation activity showed that the compounds had moderate to strong antiproliferative ability against the tested cell lines except of HL3 against the SMMC7721 cell line. The results indicated that the heterocycle attached to the norcantharidin was favorable to antiproliferative activity. This result was consistent with the DNA binding experiment.

Facile template synthesis of water-soluble triazine-based Schiff base ligand bridged-coordination polymers of Co(ii), Ni(ii), and Cu(ii): structure, biomolecular interactions, and cytotoxic activity

2019 ◽  
Vol 43 (34) ◽  
pp. 13371-13380 ◽  
Author(s):  
Sheikdawood Parveen ◽  
Thathan Premkumar ◽  
Hung Huy Nguyen ◽  
Subbiah Govindarajan
Keyword(s):  
Schiff Base ◽  
Cytotoxic Activity ◽  
Coordination Polymers ◽  
Schiff Base Ligand ◽  
Template Synthesis ◽  
Water Soluble ◽  
Biomolecular Interactions ◽  
First Time ◽  
Ct Dna

For the first time, a new hydrazone Schiff base ligand and its Co(ii), Ni(ii), and Cu(ii) complexes were synthesised and characterised. Their antioxidant and binding activities towards CT-DNA and BSA were evaluated.

Interaction of a synthesized pyrene based fluorescent probe with CT-DNA: spectroscopic, thermodynamic and molecular modeling studies

RSC Advances ◽  
2016 ◽  
Vol 6 (96) ◽  
pp. 93335-93342 ◽  
Author(s):  
Soumen Ghosh ◽  
Abdulla Al Masum ◽  
Aniruddha Ganguly ◽  
Md. Akhtarul Alam ◽  
Md. Maidul Islam ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Fluorescent Probe ◽  
Water Soluble ◽  
Calf Thymus Dna ◽  
Modeling Studies ◽  
Calf Thymus ◽  
Molecular Modeling Studies ◽  
Ct Dna

The present study demonstrates the synthesis of a new pyrene based water soluble fluorescent probe and its interaction with Calf-thymus DNA.

scholarly journals Seleninic Acid Potassium Salts as Water-Soluble Biocatalysts with Enhanced Bioavailability

Materials ◽  
2020 ◽  
Vol 13 (3) ◽  
pp. 661 ◽  
Author(s):  
Magdalena Obieziurska ◽  
Agata J. Pacuła ◽  
Anna Laskowska ◽  
Angelika Długosz-Pokorska ◽  
Anna Janecka ◽  
...  
Keyword(s):  
Glutathione Peroxidase ◽  
Anticancer Agents ◽  
Potassium Salt ◽  
Water Soluble ◽  
Potassium Salts ◽  
Organoselenium Compounds ◽  
Protic Solvents ◽  
Ros Formation ◽  
Mcf 7 ◽  
Acid Salts

Organoselenium compounds are well-known glutathione peroxidase (GPx) mimetics that possess antioxidants/prooxidant properties and are able to modulate the concentration of reactive oxygen species (ROS), preventing oxidative stress in normal cells or inducing ROS formation in cancer cells leading to apoptosis. The purpose of this study was the synthesis of potent GPx mimics with antioxidant and anticancer activity along with improved bioavailability, as a result of good solubility in protic solvents. As a result of our research, glutathione peroxidase (GPx) mimetics in the form of water-soluble benzeneseleninic acid salts were obtained. The procedure was based on the synthesis of 2-(N-alkylcarboxyamido)benzeneselenenic acids, through the oxidation of benzisoselenazol-3(2H)-ones or analogous arenediselenides with an amido group, which were further converted to corresponding potassium salts by the treatment with potassium tert-butanolate. All derivatives were tested as potential antioxidants and anticancer agents. The areneseleninic acid salts were significantly better peroxide scavengers than analogous acids and the well-known organoselenium antioxidant ebselen. The highest activity was observed for the 2-(N-ethylcarboxyamido)benzeneselenenic acid potassium salt. The strongest cytotoxic effect against breast cancer (MCF-7) and human promyelocytic leukemia (HL-60) cell lines was found for 2-(N-cyclohexylcarboxyamido)benzeneselenenic acid potassium salt and the 2-(N-ethylcarboxyamido)benzeneselenenic acid, respectively. The structure–activity correlations, including the differences in reactivity of benzeneseleninic acids and corresponding salts were evaluated.

Drug delivery of anticancer agents: water soluble 4-poly (ethylene glycol) derivatives of the lignan, podophyllotoxin

1999 ◽  
Vol 61 (3) ◽  
pp. 281-294 ◽  
Author(s):  
Richard B Greenwald ◽  
Charles D Conover ◽  
Annapurna Pendri ◽  
Yun H Choe ◽  
Anthony Martinez ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Ethylene Glycol ◽  
Anticancer Agents ◽  
Water Soluble ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
Ethylene Glycol Derivatives ◽  
Derivatives Of

Spectrophotometric Study on the Binding of Two Water Soluble Schiff Base Complexes of Mn (III) with ct-DNA

2011 ◽  
Vol 21 (4) ◽  
pp. 1649-1658 ◽  
Author(s):  
Maryam Nejat Dehkordi ◽  
Abdol-Khlegh Bordbar ◽  
Masood Ayatolahi Mehrgardi ◽  
Valiolah Mirkhani
Keyword(s):  
Schiff Base ◽  
Spectrophotometric Study ◽  
Water Soluble ◽  
Schiff Base Complexes ◽  
Ct Dna
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