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Showing 1 to 20 of 20 for “"Platinum compounds"”.
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Interactions of platinum compounds with heterocyclic bases.
It is generally accepted that platinum antitumoar drugs bind, preferentially, to Guanine N7 in DNA. Thus the kinetics of formation and the energetics of dissociation of platinum-nitrogen bonding have been investigated, using simple model bases, namely pyridine. pyrimidine. purine and some …
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A Study on the Protein Interaction with Different Platinum Compounds
… metastatic or advanced cancer with cisplatin and platinum compounds. Platinum compounds covalently bind to DNA and disrupt DNA function. They are also known to bind with amino acids like methionine, histidine and cysteine to form cisplatin-protein adducts which are responsible for most of its …
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Mechanisms of Accumulation and Biological Consequences of Polynuclear Platinum Compounds
… and cellular uptake than clinical anticancer platinum drugs such as cisplatin, oxaliplatin and carboplatin. The clinical efficacy of cisplatin, oxaliplatin and carboplatin is limited due to acquired resistance and dose limiting side effects. The three major pharmacological factors contributing …
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Non-traditional platinum compounds for improved cellular accumulation and tumor targeting
Chapter 1. Introduction to Non-Traditional Platinum Compounds for Improved Uptake, Oral Bioavailability, and Tumor Targeting The path to more potent platinum anticancer drugs with fewer side effects lies in the exploration of non-traditional platinum compounds, which do not necessarily contain the …
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Drug Design, Biological Activity, and Metabolic Consequences of Cytotoxic Platinum Compounds: Utilizing Fluorescent Tagging to Understand Drug Action and Metabolism
Platinum drugs are among the most commonly used chemotherapeutics for the treatment of testicular, head and neck, ovarian, small cell lung, and colorectal carcinomas. Although the current set of platinum chemotherapeutics has proven somewhat successful, the overall success of platinum based drugs …
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Activity of Analogs of Anticancer Drugs on the Serine Protease Enzymes Subtilisin and Chymotrypsin
<p>The anticancer activity of several platinum compounds is due to the formation of complexes with DNA. We hypothesize that the size and shape of the platinum compounds would impact interaction with proteins, and these interactions may be partly responsible for the anticancer activity. Chymotrypsin …
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Effect of Leaving Ligands of Platinum(II) Diamine Complexes on DNA and Protein Residues
<p>Platinum compounds are widely used drugs in cancer treatments. Although DNA is the biological target, reaction of platinum compounds with proteins is also potentially significant. Our objective is to study the effects of leaving ligands on the relative reactivity between 5'-GMP (guanosine 5' …
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Kinetic studies of the hydrolysis reactions of ruthenium (III) complexes hIm trans-[RuCl₄(im)₂] and hInd trans-[RUCl₄(ind)₂] by uv-visible spectrophotometry
… cancers have developed resistance towards platinum compounds. Platinum compounds have severe adverse effects that limited their use towards a wide range of tumors.</p> <p>Ruthenium complexes are considered as pro-drugs, as they transform into antitumor active species in the body by …
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High-resolution NMR spectroscopic analysis of anticancer drugs, DNA and their interactions: 1. Platinum anticancer compounds - DNA interactions. 2. Anthracycline drugs - DNA interactions and modified DNA
… devoted to designing the new better anticancer platinum compounds. The structural studies on interactions of two anticancer platinum compounds, cisplatin and the third-generation bisplatinum compound 1,1/t,t, with DNA are described in this thesis. The structure of an intrastrand …
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Synthetic strategies for the design of platinum anticancer drug candidates
Chapter 1. The Synthetic Chemistry of Platinum Anticancer Agents Since the inception of cisplatin as a clinically approved anticancer agent, a large number of platinum compounds have been synthesized with the aim of finding new, improved drugs. As a result of these efforts, only two additional …
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Cytotoxic Effects of Ruthenium Compounds on Human Cancer Cell Lines.
… the most common cancer treatment. Traditionally, platinum-based drugs are used in chemotherapy. More recently, researchers have focused on ruthenium based compounds as a substitute for the platinum compounds. Ruthenium-based compounds appear to be less toxic to healthy cells than traditional …
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Synthetic strategies to improve the cytotoxicity of platinum-based cancer therapeutics
… is to explore the conjugation of biomolecules to platinum(IV) compounds. Ever since the serendipitous discovery that cisplatin has cytotoxic properties in the 1970's, research has focused on both understanding the mode of action and making new potential drugs that have more desirable properties …
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Transcription and mismatch repair in the mechanism of action of the anticancer drug cisplatin
cis-Diamminedichloroplatinum(II) (cis-DDP or cisplatin) is a powerful cytotoxin and anticancer therapeutic, used most effectively in the treatment of testicular and ovarian cancers. By contrast, the geometric isomer of cisplatin, trans- DDP, is comparatively non-toxic and fails to show significant …
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New methodologies for studying the biological activity of platinum complexes
A review of existing approaches to platinum drug discovery highlighted the need for new methods to perform mechanism-based, high-throughput screening of platinum complexes. A new solution phase screening method was based on the importance of high mobility group (HMG) domain proteins in the …
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Disruption of Dna Polymerase Zeta Promotes An Innate Immune Response
… stresses including ultraviolet irradiation and platinum compounds such as the chemotherapeutic agent cisplatin. This elevated sensitivity arises from the central role of pol ζ in lesion bypass. Pol ζ is also required to protect cells from endogenous genomic damage or stress. In primary mammalian …
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Investigating the role of NEIL3 in colorectal cancer resistance to oxaliplatin
… and usage at tolerable doses. Like other platinum compounds such as cisplatin, the molecular target of oxaliplatin is DNA, where it produces DNA intra- and inter-strand crosslinks that prevent transcription and DNA replication to cause cell death. Although numerous mechanisms of tumour …
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Palladium and platinum complexes of vitamin Bâ
Palladium and platinum complexes of pyridoxamine, pyridoxine and pyridoxal have been prepared. The structures of the complexes PtCI2PM.H20, trans-PdC12 (PN)2 and [PLH+ ]2[PtC16] 2- ,H20 have been determined by use of single crystal x-ray studies. The compounds PdC12PH, trans-PdC12 (PN) 2 , …
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A novel mechanism for the anti-cancer activity of aspirin and its analogues
… The search for potential aspirin-related compounds with the same or better cytotoxic effects against cancer cells accompanied by a safer toxicity profile has been ongoing over the years and led to us to synthesise a number of novel aspirin analogues. One of the mechanisms of action …
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APPROACHES OF MODULATION OF THERAPEUTIC TARGETS RELEVANT TO DRUG RESISTANCE
… and motivated many groups to synthesize new compounds. The aim of this project is to identify new Hsp90 inhibitors which could overcome the limitations of available inhibitors and exhibit therapeutic advantages in terms of specificity, therapeutic index and antitumor efficacy. Several …