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DNA intercalation

Ritika S Joshi, Dipanwita Das Mukherjee, Subhendu Chakrabarty, Ansie Martin, Manojkumar Jadhao, Gopal Chakrabarti, Angshuman Sarkar, Sujit Kumar Ghosh
In the development of small molecule drug candidates, naphthalimide based compounds hold a very important position as potent anti-cancer agents with considerable safety in drug discoveries. Being synthetically and readily accessible, naphthalimide compounds with planar architecture have been developed mostly as DNA targeting intercalators. However, in this article, we demonstrate, for the first time, wherein an unfused naphthalimide-benzothiazole bichromophoric compound 2-(6-chlorobenzo[d] thiazol-2-yl)-1H-benzo[de] isoquinoline-1,3(2H)-dione (CBIQD), designed and synthesized by our group, seem to expand the bioactivity of naphthalimide as anti-mitotic agents also...
March 21, 2018: Journal of Physical Chemistry. B
Maria-Eleni Kyriazi, Davide Giust, Afaf H El-Sagheer, Peter M Lackie, Otto L Muskens, Tom Brown, Antonios G Kanaras
The design of nanoparticulate systems which can perform multiple synergistic functions in cells with high specificity and selectivity is of great importance in applications. Here we combine recent advances in DNA-gold nanoparticle self-assembly and sensing to develop gold nanoparticle dimers that are able to perform multiplexed synergistic functions within a cellular environment. These dimers can sense two mRNA targets and simultaneously or independently deliver one or two DNA-intercalating anticancer drugs (doxorubicin and mitoxantrone) in live cells...
March 20, 2018: ACS Nano
Qingyi Tong, Huijuan You, Xintao Chen, Kongchao Wang, Weiguang Sun, Yufeng Pei, Xiaodan Zhao, Ming Yuan, Hucheng Zhu, Zengwei Luo, Yonghui Zhang
Despite All-trans retinoic acid (ATRA) has transformed acute promyelocytic leukemia (APL) from the most fatal to the most curable hematological cancer, there remains a clinical challenge that many high-risk APL patients who fail to achieve a complete molecular remission or relapse and become resistant to ATRA. Herein, we report that 5-(4-methoxyphenethyl)-[1, 3] dioxolo [4, 5-j] phenanthridin-6(5H)-one (ZYH005) exhibits specific anticancer effects on APL and ATRA-resistant APL in vitro and vivo, while shows negligible cytotoxic effect on non-cancerous cell lines and peripheral blood mononuclear cells from healthy donors...
March 15, 2018: Nucleic Acids Research
Sreejesh Sreedharan, Alessandro Sinopoli, Paul J Jarman, Darren Robinson, Christopher Clemmet, Paul A Scattergood, Craig R Rice, Carl G W Smythe, James A Thomas, Paul I P Elliott
Two new biscyclometalated complexes [Ir(ptzR)2(dppz)]+ (dppz = dipyridophenazene; ptzRH = 4-phenyl-1-benzyl-1,2,3-triazole (1+) and 4-phenyl-1-propyl-1,2,3-triazole (2+)) have been prepared. The hexafluorophosphate salts of these complexes have been fully characterized and, in one case, the X-ray structure of a nitrate salt was obtained. The DNA binding properties of the chloride salts of the complexes were investigated, as well as their cellular uptake by A2780 and MCF7 cell lines. Both complexes display an increase in the intensity of phosphorescence upon titration with duplex DNA, indicating the intercalation of the dppz ligand and, given that they are monocations, the complexes exhibit appreciable DNA binding affinity...
March 19, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
Patrick O Asekunowo, Rosenani A Haque, Mohd R Razali, Silas W Avicor, Mustafa F F Wajidi
A series of four benzimidazolium based nitrile-functionalized mononuclear-Ag(I)-N-heterocyclic carbene and binuclear-Ag(I)-N-heterocyclic carbene (Ag(I)-NHC) hexafluorophosphate complexes (5b-8b) were synthesized by reacting the corresponding hexafluorophosphate salts (1b-4b) with Ag2 O in acetonitrile, respectively. These compounds were characterized by1 H NMR,13 C NMR, IR, UV-visible spectroscopic techniques, elemental analyses and molar conductivity. Additionally, 8b was structurally characterized by single crystal X-ray diffraction technique...
March 13, 2018: European Journal of Medicinal Chemistry
Bita Zamiri, Mila Mirceta, Rashid Abu-Ghazalah, Marc S Wold, Christopher E Pearson, Robert B Macgregor
BACKGROUND: Expansion of the C9orf72 hexanucleotide repeat (GGGGCC)n •(GGCCCC)n is the most common cause of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). Both strands of the C9orf72 repeat have been shown to form unusual DNA and RNA structures that are thought to be involved in mutagenesis and/or pathogenesis. We previously showed that the C-rich DNA strands from the C9orf72 repeat can form four-stranded quadruplexes at neutral pH. The cytosine residues become protonated under slightly acidic pH (pH 4...
March 14, 2018: Biochimica et Biophysica Acta
Mousumi Pal, Utpal Nandi, Debaraj Mukherjee
Ruthenium (Ru) complexes are known for their promising anticancer activity presumably due to octahedral coordination geometry, slow ligand exchange rate, the range of different oxidation states and target specificity. This review article summarizes the physicochemical processes which are responsible for the selectivity of Ru complexes toward cancer cells over the normal cells. Emphasis has been given on the activation mechanism of Ru(III) complex administered as a prodrug and then the release of active species in an acidic environment of cancer cell through normal or photo induced hydrolysis or ligand oxidation...
March 7, 2018: European Journal of Medicinal Chemistry
Qingwang Xue, Chunxue Liu, Xia Li, Li Dai, Huaisheng Wang
Various fluorescent sensing systems for miRNAs detection have been developed. But they mostly contain enzymatic amplification reactions and label procedures. The strict reaction conditions of tool enzymes and the high cost of labeling limit their potential applications, especially in complex biological matrix. Here we have addressed the difficult problems and report a strategy for label-free fluorescent DNA dendrimers based on enzyme-free nonlinear hybridization chain reaction (HCR)-mediated multiple G-quadruplex for simple, sensitive and selective detection of miRNAs with low-background signal...
March 16, 2018: Bioconjugate Chemistry
Yuan Zhang, Vijai Kumar Reddy Tangadanchu, Yu Cheng, Ren-Guo Yang, Jian-Mei Lin, Cheng-He Zhou
A series of isopropanol-bridged carbazole azoles as potential antimicrobial agents were designed and synthesized from commercial carbazoles. Bioassay revealed that 3,6-dichlorocarbazolyl triazole 3f could effectively inhibit the growth of E. faecalis with minimal inhibitory concentration of 2 μg/mL. The active molecule 3f showed lower propensity to trigger the development of resistance in bacteria than norfloxacin and exerted rapidly bactericidal ability. Compound 3f also exhibited low cytotoxicity to normal mammalian RAW264...
March 8, 2018: ACS Medicinal Chemistry Letters
Swetha K Maddili, Ramesh Katla, Vijaya Kumar Kannekanti, Naveen Kumar Bejjanki, Balaraju Tuniki, Cheng-He Zhou, Himabindu Gandham
The binding behaviour between calf thymus DNA and synthesized benzothiazolyl triazolium derivatives as potent antimicrobial agents was explored by means of spectroscopic applications together with molecular docking study at the sub-domain IIA, binding site I of human serum albumin (HSA). Most of the synthesized derivatives presented significant antimicrobial inhibition when compared with the clinical Norfloxacin, Chloromycin, and Fluconazole. In particular, compound 5q presented efficient anti-Bacillus subtilis, anti-Escherichia coli, anti-Salmonella typhi, and anti-Psuedomonas aeruginosa activity with low MIC values of 2-8 μg/mL which were relatively superior to the reference drugs...
February 21, 2018: European Journal of Medicinal Chemistry
Cheng-He Zhou, Ya-Nan Wang, Rammohan R Yadav Bheemanaboina, Wei-Wei Gao, Jie Kang, Gui-Xin Cai
A series of benzimidazole quinolone hybrids as new potential antimicrobial agents were designed and synthesized, and their bioactive assay indicated that some prepared compounds exhibited potent antibacterial and antifungal activities. Notably, 2-fluorobenzyl derivative 5b showed remarkable antimicrobial activities against the resistant P. aeruginosa and C. tropicalis isolated from infected patients. The active molecule 5b could not only rapidly kill the tested strains, but also exhibit low toxicity towards Hep-2 cells...
March 7, 2018: ChemMedChem
Thangavel Thirunavukkarasu, Hazel A Sparkes, C Balachandran, S Awale, Karuppannan Natarajan, V G Gnanasoundari
A novel one-dimensional coordination polymer containing Cu(I)Cu(II) core with chloro bridge on Cu(I) and ligand bridge on Cu(II) ions (1) and a mononuclear Cu(II) complex (2) have been synthesized from the reactions of 3- and 4-methoxy-3-quinolin-3-ylimino-methyl-2-phenol with [CuCl2 (PPh3 )2 ]. The ligands and the complexes have been characterized by spectral and analytical methods. In addition, the structures of both the ligands and the copper complexes were confirmed by single crystal X-ray diffraction studies...
February 13, 2018: Journal of Photochemistry and Photobiology. B, Biology
Maryam Sedighipoor, Ali Hossein Kianfar, Mohammad R Sabzalian, Fatemeh Abyar
Two novel tetra-coordinated Cobalt(II) and Zinc (II) chelate series with the general formula of [Co (L)·2H2 O] (1) and [Zn (L)] (2) [L=N-2-hydroxyacetophenon-N'-2-hydroxynaphthaldehyde-1,2 phenylenediimine)] with biologically active Schiff base ligands were synthesized and recognized by elemental analysis and multi-nuclear spectroscopy (IR and1 H and13 C NMR); then, their biological activities including DNA and protein interactions were studied. The interaction of the synthesized compounds with bovine serum albumin (BSA) was investigated via fluorescence spectroscopy, showing the affinity of the complexes for these proteins with relatively high binding constant values and the changed secondary BSA structure in the presence of the complexes...
February 21, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Eda Yuhana Ariffin, Yook Heng Lee, Dedi Futra, Ling Ling Tan, Nurul Huda Abd Karim, Nik Nuraznida Nik Ibrahim, Asmat Ahmad
A novel electrochemical DNA biosensor for ultrasensitive and selective quantitation of Escherichia coli DNA based on aminated hollow silica spheres (HSiSs) has been successfully developed. The HSiSs were synthesized with facile sonication and heating techniques. The HSiSs have an inner and an outer surface for DNA immobilization sites after they have been functionalized with 3-aminopropyltriethoxysilane. From field emission scanning electron microscopy images, the presence of pores was confirmed in the functionalized HSiSs...
March 5, 2018: Analytical and Bioanalytical Chemistry
Brendan G Dwyer, Emily Johnson, Efren Cazares, Karen L McFarlane Holman, Sarah R Kirk
The ruthenium-based anticancer agent NAMI-A (ImH[trans-RuCl4 (dmso)(Im)], where Im = imidazole) has been shown to interact with RNA in vivo and in vitro. We hypothesized that the similarly structured drug KP1019 (IndH[trans-RuCl4 (Ind)2 ], where Ind = indazole) binds to RNA as well. Fluorescence spectroscopy was employed to assay the interactions between either NAMI-A or KP1019 and tRNAPhe through an intrinsic fluorophore wybutosine (Y) base and by extrinsic displacement of the intercalating agent ethidium bromide...
February 24, 2018: Journal of Inorganic Biochemistry
Xinran Geng, Yichang Ren, Fangfang Wang, Danmei Tian, Xinsheng Yao, Youwei Zhang, Jinshan Tang
Harmine and its analogs have long been considered as anticancer agents. In vitro analyses suggested that intercalating DNA or inhibiting topoisomerase might contribute to the cytotoxic effect of this class of compound. However, this idea has not been rigorously tested in intact cells. By synthesizing novel derivatives, here we demonstrate that harmines did not activate the DNA damage response, a cellular signaling commonly induced by agents that intercalate DNA or inhibit topoisomerase. These findings suggest that mechanisms other than DNA intercalating or topoisomerase inhibiting contribute to the toxicity of harmines in vivo...
February 28, 2018: Biochemical and Biophysical Research Communications
M K Islam, P J M Jackson, D E Thurston, K M Rahman
We report a series of novel methylene-linked bis-phenylbenzimidazoles intercalators that stabilize telomeric DNA/RNA hybrid (tDRH) structures by up to 7.2 °C at a 1 μM ligand concentration while having negligible affinity for DNA/DNA duplexes, although with a low affinity for quadruplex DNA. We have used molecular modelling studies to rationalize this selectivity, concluding that the methylene spacer between the terminal benzimidazole and phenylene moieties plays a key role in facilitating the bis-intercalating process...
March 2, 2018: Organic & Biomolecular Chemistry
Bappa Maiti, Mohini Kamra, Anjali A Karande, Santanu Bhattacharya
Herein, five new α-tocopheryl cationic gemini lipids with hydroxyethyl bearing headgroups (THnS, n = 4, 5, 6, 8, 12) have been synthesized for efficient plasmid DNA (pDNA) delivery into cancer cells. Among these gemini lipid formulations, the lipid with an octamethylene [-(CH2 )8 ] spacer (TH8S) showed the highest transfection efficiency (TE) that was comparable to that of the commercial standard lipofectamine 2000 (L2K) in terms of luciferase expression in HepG2 (liver hepatocellular carcinoma) cells. The addition of the helper lipid DOPE (1,2-dioleoyl phosphatidyl ethanolamine) with cationic lipids in mixed liposomes further enhanced the TE and the optimized molar ratio was 2 : 1 (DOPE : cationic lipid)...
March 2, 2018: Organic & Biomolecular Chemistry
Rashmi Gupta, Carolina R Felix, Matthew P Akerman, Kate J Akerman, Cathryn A Slabber, Wenjie Wang, Jessie Adams, Lindsey N Shaw, Yuk-Ching Tse-Dinh, Orde Q Munro, Kyle H Rohde
Mycobacterium tuberculosis ( Mtb ) and the fast-growing Mycobacterium abscessus ( Mab ) are two important human pathogens causing persistent pulmonary infections that are difficult to cure and require long treatment times. The emergence of drug resistant Mtb strains and the high level of intrinsic resistance of Mab calls for novel drug scaffolds that effectively target both pathogens. In this study, we have evaluated the activity of bis(pyrrolide-imine) gold(III) macrocycles and chelates, originally designed as DNA intercalators capable of targeting human topoisomerase I and II, against Mab and Mtb...
February 26, 2018: Antimicrobial Agents and Chemotherapy
Eimer Mary Tuite, Bengt Norden
The assembly of stacked dyes on DNA is of interest for electron transfer, light harvesting, sensing and catalysis applications. A combination of UV/vis absorption, linear dichroism (LD), and circular dichroism (CD) was applied to characterize thoroughly the aggregation with DNA of the phenothiazine dyes methylene blue, azure B, and thionine. Aggregates of each dye with [poly(dG-dC)]2 , [poly(dA-dT)]2 and calf thymus DNA were explored at high dye:DNA binding ratios, where excess dye groove-binds after all intercalation sites are filled...
February 26, 2018: Journal of Physical Chemistry. B
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