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Chemical Biology & Drug Design

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https://www.readbyqxmd.com/read/28524273/synthesis-and-biological-evaluation-of-novel-peptides-based-on-antimicrobial-peptides-as-potential-agents-with-anti-tumor-and-multidrug-resistance-reversing-activities
#1
Bo Zhang, Wei Shi, Jieming Li, Chen Liao, Limei Yang, Wenlong Huang, Hai Qian
Tumor chemotherapy, which plays an important role in the clinical treatment of metastatic cancer, is limited by low selectivity and drug resistance in clinical application. In our study, we selected antimicrobial peptide BP100 as a lead peptide, designed and synthesized a series of novel antineoplastic peptides through solid-phase synthesis. Amongst them, B4 and B8 showed excellent anti-cancer activity. As revealed by further investigations, these peptides could disrupt the cell membrane, trigger the cytochrome C release into cytoplasm and ultimately lead to apoptosis...
May 19, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28509385/molecular-events-leading-to-death-of-leishmania-donovani-under-spermidine-starvation-after-hypericin-treatment
#2
Shalini Singh, Ekta Kumari, Ruchika Bhardwaj, Ritesh Kumar, Vikash Kumar Dubey
We have previously reported that the hypericin treatment caused spermidine starvation and death of Leishmania parasite. Here, we report different molecular events under spermidine starvation and potential role of spermidine in processes other than redox homeostasis of the parasite. We have analyzed changes in expression of several genes by using quantitative gene expression analysis. Further, these changes at molecular level were also confirmed by using biochemical and cellular studies. Altered expression of several genes involved in redox metabolism, hypusine modification of eIF5A, DNA repair pathway and autophagy was observed...
May 16, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28498641/quaternary-ammonium-salts-substituted-by-5-phenyl-1-3-4-oxadiazole-2-thiol-as-novel-antibacterial-agents-with-low-cytotoxicity
#3
Chun-Hua Wang, Xian-Rui Xie, Wen-Shuai Liu, Gui-Ge Hou, Ju-Feng Sun, Feng Zhao, Wei Cong, Hong-Juan Li, Wen-Yu Xin
Twenty-one novel 5-phenyl-1,3,4-oxadiazole-2-thiol (POT) substituted N-hydroxyethyl quaternary ammonium salts (6a-g, 7a-g, 8a-g) were prepared and characterized by FTIR, NMR and elemental analysis. Compounds 6a, 6c and 8a were confirmed by X-ray single-crystal diffraction. They display the unsurpassed antibacterial activity against S. aureus, α-H-tococcus, E. coli, P. aeruginosa, Proteus vulgaris, Canidia Albicans, especially 6g, 7g, 8g with dodecyl group. Compounds 8a-d with N,N-dihydroxyethyl and POT groups display unsurpassed antibacterial activity and nontoxicity...
May 12, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28498511/enhanced-antitumor-effect-of-targeted-nanoliposomal-bleomycin
#4
Mohsen Chiani, Kayhan Azadmanesh, Mohammad Ali Shokrgozar, Mohammad Reza Mehrabi, Azim Akbarzadeh, Dariush Norouzian
Folate receptor (FR)-mediated drug delivery is a promising approach for active targeting of drugs to the FR-positive tumor cells. Bleomycin (BLM) is an antitumor antibiotic with poor therapeutic activity as a result of its limited diffusion into tumor cells. The aim of this study was to investigate whether FR-targeted PEGylated nanoliposomes (FPNL) can effectively deliver BLM to tumor cells and enhance its in vitro and in vivo efficacy. FPNL and PNL (non-targeted) were prepared by thin film hydration method and their physiochemical properties, cellular uptake, tissue distribution and tumor inhibitory effects were investigated...
May 12, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28489280/synthesis-and-evaluation-of-cytotoxic-activities-of-artemisinin-derivatives
#5
Qian Sun, Jin Wang, Yao Li, Jingjing Zhuang, Qian Zhang, Xiao Sun, Dequn Sun
Artemisinin is naturally occurring antimalarials which has shown potent anticancer activity. In the present work, a new kind of artemisinin derivatives with piperazino group were synthesized. The cytotoxic activities of derivatives 5a-5d were evaluated by MTT assay against ten cell lines. The result showed that 5a-5d were more effective in inhibiting cancer cells growth than artemisinin. 5d was the most active against HepG2 and PLC-PRF-5 cells, and presented no cytotoxicity on L-02 cells. Hoechst33342 staining and flow cytometry experiment revealed that 5d could induce HepG2 and PLC-PRF-5 cells apoptosis...
May 10, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28489276/design-synthesis-and-preliminary-bioactivity-evaluation-of-n-benzylpyrimidin-2-amine-derivatives-as-novel-histone-deacetylase-hdac-inhibitor
#6
Yi Zhou, Yanyan Dun, Huansheng Fu, Lei Wang, Xiaole Pan, Xinying Yang, Hao Fang
Histone deacetylase inhibitors have been identified for the treatment of cancer. Lately, we designed and synthesized a series of substituted N-benzylpyrimidin-2-amine derivatives as potent HDAC inhibitors. In vitro HDAC inhibitory activities and anti-proliferative activities of target compounds were investigated. Some target compounds showed potent HDAC inhibitory activities and possessed obvious anti-proliferative activity against tumor cells. Target compounds 6a, 6d, 8a, 8c and 8f not only exhibited almost equally enzymatic inhibitory activity with SAHA, but showed better anti-proliferative activities...
May 10, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28489275/recent-drug-therapies-for-corneal-neovascularization
#7
REVIEW
Xinyao Liu, Shurong Wang, Xuanzhong Wang, Jiaming Liang, Yan Zhang
Corneal neovascularization (CNV) is a common pathological change in ocular surface diseases. It is not only the factor that affects vision, but also the main cause for corneal graft failure. Based on the mechanism of CNV, many achievements have been developed to suppress the formation of CNV. There are certain novel drugs such as aflibercept, gold nanoparticles and netrins which provide us with new clues to treat CNV. However, we still need to develop more effective therapeutic drugs. It is of great significance to develop new effective drugs to suppress the occurrence of CNV...
May 10, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28459507/molecular-recognition-of-a-carboxy-pyridostatin-towards-g-quadruplex-structures-why-does-it-prefer-rna
#8
Roberta Rocca, Carmine Talarico, Federica Moraca, Giosuè Costa, Isabella Romeo, Francesco Ortuso, Stefano Alcaro, Anna Artese
The pyridostatin (PDS) represents the lead compound of a family of G-quadruplex (G4) stabilizing synthetic small molecules based on a N,N'-bis(quinolinyl)pyridine-2,6-dicarboxamide scaffold. Its mechanism of action involves the induction of telomere dysfunction by competing for binding with telomere associated proteins, such as human POT1. Recently, through a template-directed 'in situ' click chemistry approach, a PDS derivative, the carboxypyridostatin (cPDS), was discovered. It has the peculiarity to exhibit high molecular specificity for RNA over DNA G4, while PDS is a good generic RNA and DNA G4-interacting small molecule...
April 29, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28459499/potential-biological-targets-for-bioassay-development-in-drug-discovery-of-sturge-weber-syndrome
#9
REVIEW
Fatemeh Mohammadipanah, Fatemeh Salimi
Sturge-Weber Syndrome (SWS) is among the neurocutaneous diseases, which has several clinical manifestations of ocular (glaucoma), cutaneous (port-wine stain), neurological (seizures) and vascular problems. Molecular mechanisms of SWS pathogenesis are initiated by the somatic mutation in GNAQ. Therefore, no definite treatments exist for the SWS and treatment options only mitigate the intensity of its clinical manifestations. Biological assay design for drug discovery against this syndrome demands comprehensive knowledge on mechanisms which are involved in its pathogenesis...
April 29, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28456998/new-insights-into-antidiabetic-drugs-possible-applications-in-cancer-treatment
#10
REVIEW
Vahid Shafiei-Irannejad, Nasser Samadi, Roya Salehi, Bahman Yousefi, Nosratollah Zarghami
Globally at 2014 it was estimated that there was 347 million people with diabetes in which 90 percent of them were diagnosed with type 2 diabetes mellitus (T2DM). Although the association between diabetes mellitus and cancer risk was found about 100 years ago, the issue is not still clear. Many studies especially cohort and case control studies have suggested a higher risk of cancer in patients with diabetes mainly in those with type 2 diabetes. Insulin concentration is high in these patients and due to its mitogenic effects it may be a possible hypotheses for higher risk of cancer in diabetic patients...
April 29, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28453915/documenting-and-harnessing-the-biological-potential-of-molecules-in-distributed-drug-discovery-d3-virtual-catalogs
#11
Milata M Abraham, Ryan E Denton, Richard W Harper, William L Scott, Martin J O'Donnell, Jacob D Durrant
Virtual molecular catalogs have limited utility if member compounds are (1) difficult to synthesize or (2) unlikely to have biological activity. The Distributed Drug Discovery (D3) program addresses the synthesis challenge by providing scientists with a free virtual D3 catalog of 73,024 easy-to-synthesize N-acyl unnatural α-amino acids, their methyl esters, and primary amides. The remaining challenge is to document and exploit the bioactivity potential of these compounds. In the current work, a search process is described that retrospectively identifies all virtual D3 compounds classified as bioactive hits in PubChem-cataloged experimental assays...
April 28, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28440951/concluding-the-trilogy-the-interaction-of-2-2-dihydroxy-benzophenones-and-their-carbonyl-n-analogues-with-human-glutathione-transferase-m1-1-face-to-face-with-the-p1-1-and-a1-1-isoenzymes-involved-in-mdr
#12
Nikolaos D Georgakis, Dionisis A Karagiannopoulos, Trias N Thireou, Elias E Eliopoulos, Nikolaos E Labrou, Petros G Tsoungas, Michael N Koutsilieris, Yannis D Clonis
The conjugation of intracellular glutathione (GSH) with several electrophilic, predominantly hydrophobic, endogenous and xenobiotic compounds, such as chemotherapeutics and carcinogenics, agrochemicals and other drugs, is catalyzed by the multigene enzyme family of glutathione transferases (GSTs). The mammalian family of GSTs comprises three groups: cytosolic, mitochondrial and microsomal. Human cytosolic GSTs constitute the largest family, which is classified in seven distinct classes named Alpha (Α), Mu (M), Pi (P), Theta (T), Sigma (S), Zeta (Z) and Omega (O)...
April 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28440948/novel-reduction-sensitive-micellar-nanoparticles-assembled-from-rituximab-doxorubicin-conjugates-as-smart-and-intuitive-drug-delivery-systems-for-the-treatment-of-non-hodgkin-s-lymphoma
#13
Huabin Yin, Tong Meng, Ling Shu, Min Mao, Lei Zhou, Haiyan Chen, Dianwen Song
In this study, a novel reduction-sensitive drug delivery system, the Rituximab-Doxorubicin (RTX-DOX) micellar nanoparticle (RDMN), was specially designed for targeted delivery and release of DOX in Non-Hodgkin's Lymphoma (NHL) cells. The RDMN was fabricated by self-assembling of amphiphilic RTX-DOX conjugates (RDCs), which were synthesized by conjugating the hydrophilic Fab fragments of RTX (an anti-CD20 monoclonal antibody) and hydrophobic DOXs by a reduction-responsive linker, 3-(2-Pyridyldithio) propionyl hydrazide (PDPH)...
April 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28434186/new-thiourea-and-1-3-thiazolidin-4-one-derivatives-effective-on-the-hiv-1-virus
#14
Anna Bielenica, Giuseppina Sanna, Silvia Madeddu, Marta Struga, Michał Jóźwiak, Anna E Kozioł, Aleksandra Sawczenko, Ilona B Materek, Alessandra Serra, Gabriele Giliberti
Thiourea derivatives have been reported to possess many biological activities, among them antiviral and antitumoral properties. As part of our continuing effort to develop new active compounds, we report the synthesis and the evaluation of new fifteen thiourea derivatives with 1,3-benzothiazol-2-yl moiety, among them a group of biologically active (1-7) also underwent cyclisation to 1,3-thiazolidin-4-ones. Molecular structure of four compounds (4, 13, 15 and 3a) was determined by an X-ray crystallography. We here report the evaluation of their cytotoxicity against human leukaemia/lymphoma- and solid tumour-derived cell lines and of their antiviral activity against HIV-1 and representatives of ssRNA and dsDNA viruses...
April 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28432813/targeting-on-poly-adp-ribose-polymerase-activity-with-dna-damaging-hybrid-lactam-steroid-alkylators-in-wild-type-and-brca1-mutated-ovarian-cancer-cells
#15
Dimitrios T Trafalis, Aikaterini Polonifi, Panayiotis Dalezis, Nikolaos Nikoleousakos, Sotirios Katsamakas, Vassiliki Sarli
Conjugated lactam-steroid alkylators (LSA), have been shown to exhibit superior activity at controlling cancer models and overlap drug resistance to conventional chemotherapy. Hybrid LSAs combine two active compounds in a single molecule and incorporate modified steroids bearing lactam moiety in one or more steroid rings functioning as vectors for cytotoxic agents. We first describe a novel class of LSAs that generate excellent anticancer activity against UWB1.289 and UWB1.289+BRCA1 human ovarian cancer cell lines...
April 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28432812/preparation-characterization-and-in-vivo-study-of-rhein-solid-lipid-nanoparticles-for-oral-delivery
#16
Haiyang Feng, Yuping Zhu, Zhixuan Fu, Dechuan Li
In this study, rhein-SLNs were successfully produced by hot homogenization followed by ultrasonication. Precirol ATO5 in which Rhein exhibited higher partition coefficient was selected for preparation of SLNs. In the dynamic light scattering, the rhein SLNs showed a smaller size with a mean value of 120.8 ± 7.9 nm and with zeta potential of -16.9 ± 2.3 mV. SLNs exhibited a good stability during the period of 2 months. The SLNs indicated faster drug release with a burst release within 2 hours and followed by a sustained release with a biphasic drug release pattern...
April 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28432753/identification-of-indothiazinone-as-a-natural-antiplatelet-agent
#17
Chansik Yang, Sugyeong Kwon, Se-Jong Kim, Minseon Jeong, Ji-Young Park, Dongeun Park, Soon Jun Hong, Jong-Wha Jung, Chungho Kim
Cardiovascular disease, which is caused by unregulated platelet aggregation, is one of the main causes of deaths worldwide. Many studies have focused on natural products with antiplatelet effects as a safe alternative therapy in order to prevent the disease. In this context, an in-house chemical library was screened to find natural products capable of inhibiting the interaction between platelet integrin αIIbβ3 and fibrinogen, which is an essential step in platelet aggregation. On the basis of the screening results, indothiazinone, an alkaloid found in microbial cultures, was identified as a potential antiplatelet agent...
April 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28419786/toward-the-rational-design-of-macrolide-antibiotics-to-combat-resistance
#18
Anna Pavlova, Jerry M Parks, Adegboyega K Oyelere, James C Gumbart
Macrolides, one of the most prescribed classes of antibiotics, bind in the bacterial ribosome's polypeptide exit tunnel and inhibit translation. However, mutations and other ribosomal modifications, especially to the base A2058 of the 23S rRNA, have led to a growing resistance problem. Here, we have used molecular dynamics simulations to study the macrolides erythromycin and azithromycin in wild-type, A2058G-mutated, and singly or doubly A2058-methylated E. coli ribosomes. We find that the ribosomal modifications result in less favorable interactions between the base 2058 and the desosamine sugar of the macrolides, as well as greater displacement of the macrolides from their crystal structure position, illuminating the causes of resistance...
April 17, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28419754/a-field-based-disparity-analysis-of-new-1-2-5-oxadiazole-derivatives-endowed-with-antiproliferative-activity
#19
Federica Porta, Arianna Gelain, Daniela Barlocco, Nicola Ferri, Silvia Marchianò, Valentina Cappello, Livia Basile, Salvatore Guccione, Fiorella Meneghetti, Stefania Villa
A series of 1,2,5-oxadiazoles was synthesized as new potential antiproliferative agents. The in vitro cytotoxic activity evaluation of title compounds through MTT-assay revealed that some of them showed significant activity against the HCT-116 cancer cell line. The field-based disparity analysis provided indications about the electrostatic, hydrophobic and shape features underlying the cytotoxicity, suggesting that increasing the negative electrostatic field on the heterocyclic core of the structure has positive effects on the activity...
April 17, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28419717/ligand-recognition-properties-of-the-vasopressin-v2-receptor-studied-under-qsar-and-molecular-modeling-strategies
#20
Marlet Martínez-Archundia, Brenda Colín-Astudillo, L M Moreno-Vargas, G Ramírez-Galicia, R Garduño-Juárez, O Deeb, Martha C Contreras-Romo, A Quintanar-Stephano, Edgar Abarca-Rojano, José Correa-Basurto
The design of new drugs that target vasopressin 2 receptor (V2R) is of vital importance to develop new therapeutic alternatives to treat diseases such as heart failure, polycystic kidney disease, etc. To get structural insights related to V2R-ligand recognition, we have used a combined approach of docking, molecular dynamics simulations (MD) and quantitative structure-activity relationship (QSAR) to elucidate the detailed interaction of the V2R with 119 of its antagonists. The three-dimensional model of V2R was built by threading methods refining its structure through MD simulations upon which the 119 ligands were subjected to docking studies...
April 17, 2017: Chemical Biology & Drug Design
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