The Anticancer Properties of Novel Platinum(II) Complexes PDF Download
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Author: Brittany Miles
Publisher:
ISBN:
Category : Cancer
Languages : en
Pages : 102
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Author: Brittany Miles
Publisher:
ISBN:
Category : Cancer
Languages : en
Pages : 102
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Author: Alyssa Patterson
Publisher:
ISBN:
Category :
Languages : en
Pages : 82
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Author: Hanni Adel Darwish
Publisher:
ISBN:
Category : Antineoplastic agents
Languages : en
Pages : 96
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Author: Atta-ur- Rahman
Publisher: Bentham Science Publishers
ISBN: 1608051617
Category : Medical
Languages : en
Pages : 792
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Book Description
"Frontiers in Anti-Cancer Drug Discovery" is an Ebook series devoted to publishing the latest and the most important advances in Anti-Cancer drug design and discovery. Eminent scientists write contributions on all areas of rational drug design and drug di
Author: Yuen-Ting Shum
Publisher: Open Dissertation Press
ISBN: 9781361428108
Category :
Languages : en
Pages :
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This dissertation, "Functionalized Platinum (II) and Gold (I) Acetylide Complexes: Structural and Spectroscopic Properties and Anticancer Activities" by Yuen-ting, Shum, 岑婉婷, was obtained from The University of Hong Kong (Pokfulam, Hong Kong) and is being sold pursuant to Creative Commons: Attribution 3.0 Hong Kong License. The content of this dissertation has not been altered in any way. We have altered the formatting in order to facilitate the ease of printing and reading of the dissertation. All rights not granted by the above license are retained by the author. Abstract: Abstract of thesis entitled FUNCTIONALIZED PLATINUM(II) AND GOLD(I) ACETYLIDE COMPLEXES. STRUCTURAL AND SPECTROSCOPIC PROPERTIES AND ANTICANCER ACTIVITIES Submitted by SHUM YUEN TING For the degree of Doctor of Philosophy at The University of Hong Kong in April 2007 Planar [Pt(terpy)X] complexes (terpy = 2,2':6',2''-terpyridine; X = Cl, SR) have frequently been cited as classic DNA metallointercalators in bioinorganic chemistry; + however, application studies of [Pt(terpy)L] (L = monoanionic ligand) and its derivatives in metal-based therapeutics are limited. In this work, a series of platinum(II) terpyridine complexes containing different glycosylated acetylide and arylacetylide ligands were prepared and characterized, the photophysical properties of which were investigated. A low-energy absorption band at 409-476 nm, which was assignable to a MLCT transition was observed in its electronic absorption spectra. Upon photoexcitation, intense emission bands at 513-733 nm were observed and were believed to originate from the excited states of 3 3 MLCT and LLCT character. Cytotoxic activities of the ''Pt(terpy)(glycosylated arylacetylide)'' system with significant inhibitory effect toward a series of carcinoma cell lines were discovered. [Pt( Bu terpy)(L3)](CF SO ) (L3 = 4-ethynylphenoxy 3 3 3 -2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside) (IC = 0.06-0.1 M) was found to be 50 i260-fold more effective in growth inhibition of the human brain cancer cell line (SF-268) than cisplatin. The binding interactions of selected platinum(II) complexes 4 5 -1 3 to calf-thymus DNA featured binding constants of 10-10 mol dm . Significantly, the spectral data were found to support a specific binding mode at the AT sequences of DNA for selected complexes. The results of cytometry experiments showed that [Pt( Bu terpy)(L3)](CF SO ) 3 3 3 induce 52.4% apoptosis in NCI-H460 cells. Based on microarray and Western blotting analyses, down-regulation of anti-apoptotic proteins, including Bcl-2 and caspase-3, were observed for platinum-treated NCI-H460 cells. When taken together, the [Pt( Bu terpy)(L3)](CF SO)-induced apoptosis in NCI-H460 cells should 3 3 3 normally occur via the mitochondrial pathway. A family of mono- and binuclear Cy P-supported gold(I) complexes which contained various π-conjugated arylacetylide ligands, were prepared and characterized. The lowest-energy singlet transitions were predominately intraligand in nature and exhibited both phenyl and acetylenic (ππ*) character. The organic triplet emissions of arylacetylide groups were thus "illuminated" at ambient conditions by ligation to the [Au(PCy )] fragment. Strong photoluminescence was detected in solid and solution states of the gold(I) complexes under ambient conditions with lifetimes in the microsecond regime. Selected gold(I) complexes were also subjected to cytotoxicity analysis; only [Au(PCy )(C≡CC H )] showed cytotoxicities (IC = 3 10 7 50 4.9-14.5 M) that were comparable to clinical cisplatin. An acetylide ligand that was appended with lomefloxacin moiety was coordinated to ii with gold(I) and platinum(II) complexes to form [CyPAu(lome)] and [Pt( Bu tpy)(lome)] (CF SO ) (lome = modified lomefloxacin), both of which were 3 3 3 structurally characterized. Tw
Author: Liliya G. Nikolcheva
Publisher:
ISBN:
Category : Platinum compounds
Languages : en
Pages : 102
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Author: Angela Casini
Publisher: Royal Society of Chemistry
ISBN: 1788017676
Category : Science
Languages : en
Pages : 370
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Book Description
Metal-based anticancer drugs are among the most successful therapeutic agents, as evidenced by the frequent prescription of selected platinum and arsenic compounds to patients. Metal-based Anticancer Agents covers the interdisciplinary world of inorganic drug discovery and development by introducing the most prominent compound classes based on different transition metals, discussing emerging concepts and enabling methods, as well as presenting key pre-clinical and clinical aspects. Recent progress on the unique features of next-generation targeted metal-based anticancer agents, including supramolecular coordination complexes used for both therapy and drug delivery, promise a bright future beyond the benefits of pure cytotoxic activity. With contributions from global leaders in the field, this book will serve as a useful reference to established researchers as well as a practical guide to those new to metallodrugs, and postgraduate students of medicinal chemistry and metallobiology.
Author: T.A. Connors
Publisher: Springer Science & Business Media
ISBN: 3642493068
Category : Medical
Languages : en
Pages : 232
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Book Description
It was a great pleasure and honour to have been invited to attend this Seminar and to present a final impression. The association in this field between the Chester Beatty Research Institute and Dr. Rosenberg's School at East Lansing is something which I specially value and many would doubtless like to know how it came about. In the course of its work in carcinogenesis and on chemotherapy over many years, the Chester Beatty Research Institute was frequently drawn to the importance of many metals - as for example lead, iron, metalloid arsenic and the metalloid quali ties of the carcinogenic hydrocarbons. Interest started in platinum many years ago, following the possibility, c1aimed by others, that various complexes between the metal and mercaptopurine might possess significant chemotherapeutic properties. Va rious attempts to confirm such findings ended, however, in complete failure. Interest in platinum was revived by the fresh observations of Dr. Rosenberg and his collea gues, and here the outcome was entirely different. Very soon it was possible to con firm the intense growth-inhibitory properties of cis-platinum (II) diamminedi chloride and related substances. After communicating these results to Dr. Rosenberg, it was a pleasure to welcome hirn in London where he gave a Seminar which greatly engaged the interest of many of the staff. Later, several of these were to enjoy Dr. Rosenberg's hospitality at an international conference on the subject to be held in East Lansing, where many rapidly developing aspects were open for discussion.
Author: Stephen B. Howell
Publisher: Springer Science & Business Media
ISBN: 030644027X
Category : Medical
Languages : en
Pages : 563
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Taken together the data presented in this review, and work by many other investigators, support the notion that DNA excision repair is important in a tumor cell's resistance to platinum compounds. Inhibition of this repair system by combination chemotherapy with the excision repair inhibitors HU and Ara-C produces synergistic cell kills and increased levels and persistance of DNA interstrand crosslinks. The studies with cis-DDP and ~-DDP in combination with UV induced thymine dimers suggest that there may be competition for DNA repair enzymes between the dimer and the platinum lesion. Whether the competing lesion is an intrastrand crosslink, interstrand crosslink, or platinum monoadduct (or all of these lesions) cannot be determined. The similarity between an intrastrand crosslink and a cyclobutane dimer suggests that these lesions may compete for repair. However, the increased peak levels of interstrand crosslinks, and increased persistence of these lesions at later time points suggest that this lesion may also be a substrate for the repair system. These observations may be of clinical relevance. Recently Dr. Kathy Albain of our institution has completed a Phase III I study using a 12 hour pretreatment with HU and Ara-C in patients prior to their cis-DDP therapy. She observed a significant number of responders in this trial (54). She is currently completing a second Phase IIII study substituting IV HU for the oral formulation. We anticipate initiating other clinical trials based upon these observations.
Author: Sinéad O'Carroll
Publisher:
ISBN:
Category :
Languages : en
Pages : 0
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Book Description
Recently, there has been major interest in the design and development of therapeutic polynuclear platinum(II) complexes (PPCs). The potential use for these complexes has been epitomised by BBR3464-a trinuclear platinum(II) complex featuring trans geometry with platinum(II) centres separated by 1,6hexanediamine linkers and terminal trans labile chloride ligands-which was the first and only platinum(II) drug to enter clinical trials not based on the conventional mononuclear cis-chemotype. While this drug class has excellent therapeutic potential, issues regarding off-target toxicity cannot be overlooked. This thesis presents the synthesis, characterisation, cytotoxic analyses, and DNA binding studies of a novel azide-appended polynuclear platinum(II) complex series (N3 -PPCs). These agents feature fully trans-symmetric geometry, vary in nuclearity, and contain a terminal azide to enable biological tracking. Furthermore, although each platinum(II) centre is separated by a 1,6hexanediamine linker similar to BBR3464, this series lack a labile chloride ligand and bind with DNA through a non-covalent mechanism called the phosphate clamp. The stand-out complex in this series, N3 -TriplatinNC, has demonstrated excellent anticancer properties in-vitro in MDA-MB-231 triple negative breast cancer cells and displays impressive in-vivo tumour regression in mice bearing MDA-MB-231 xenografts. Click chemistry labelling studies were conducted to investigate the cellular localisation and accumulation properties of the N3 -PPC series in MDA-MB-231 triple negative breast cancer cell lines. This method of post-exposure 'click' modification facilitates accurate detection of the localisation and accumulation properties of the native drug alone. Finally, azide-appended PPCs were functionalised with a thiazole orange (TO) reporter molecule to create the N3 -TO-PPC series. These TO-appended N3 -PPCs were studied for their DNA binding properties and results were compared to the aforementioned N3 -PPCs and earlier reported PPCs. Future work on the TO appended PPCs entails cellular tracking within MDA-MB-231 cell lines and compared to non-TO modified congeners.
