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Medicinal Chemistry

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https://www.readbyqxmd.com/read/28629311/cell-cycle-arrest-and-apoptosis-induction-activity-of-nitidine-chloride-on-acute-myeloid-leukemia-cells
#1
Peng Li, Shuxin Yan, Xin Dong, Zhao Li, Yu Qiu, Chunyan Ji, Jingru Zhang, Min Ji, Wei Li, Hongchun Wang, Zhi Liu, Xing Li Wang, Jingjing Ye, Daoxin Ma
: Background: Acute myeloid leukemia (AML) is the most common hematological malignancy in adults, characterized by distorted proliferation and development of myeloid cells and their precursors in the bone marrow. Nitidine chloride, a naturally occurring alkaloid, has been identified to possess antitumor activity. However, the effects of nitidine chloride on acute myeloid leukemia cells and its underlying mechanisms have not been elucidated. Here we investigated the cellular and molecular mechanism of the anti-leukemic effects of nitidine chloride...
June 19, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28606042/isolation-of-chlorogenic-acid-from-soil-borne-fungi-screlotium-rolfsii-their-reversal-of-multidrug-resistance-and-anti-proliferative-in-mouse-lymphoma-cells
#2
Bashir Ahmad, Muhammad Rizwan, Abdur Rauf, Muslim Raza, Shumaila Bashir, Joseph Molnáre, Ákos Csonka, Diána Szabó, Mohammad S Mubarak, Mah Noor, Bina S Siddiqui
BACKGROUND: Fungi performing a wide range of function in soil by secreting low molecular weight compound known as secondary metabolites. S. rolfsii is a soil borne phytopathogenic fungi was used for the production of bioactive compounds. OBJECTIVE: The present study belongs to evaluate the anticancer potentials of a secondary metabolites isolated from S. rolfsii, their multidrug resistance (MDR), and molecular docking study. METHOD: (1S,3R,4R,5R,E)-3-(3-(3,4-Dihydroxyphenyl)acryloyloxy)-1,4,5 trihydroxycyclohexanecarboxylic acid (1), or best known as chlorogenic acid, was isolated from the ethyl acetate fraction of crude secondary metabolites produced by the soil borne Fungus Screlotium rolfsii...
June 12, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28571532/rapid-access-to-oxazine-fused-furocoumarins-and-in-vivo-and-in-silico-studies-of-theirs-biological-activity
#3
Alla V Lipeeva, Dmitry S Baev, Margarita P Dolgikh, Tatijana G Tolstikova, Elvira E Shults
BACKGROUND: The synthesis of 1,2-oxazine-fused linear furocoumarins was performed involving the transition metal catalysis reaction of plant coumarin oreoselone derivatives. OBJECTIVE AND METHODS: The Pd-catalyzed desulfonative cross-coupling reactions of 2-(tosyl)oreoselone with terminal alkynes and the successive treatment of the obtained 2-(arylethynyl)furocoumarins with an excess of hydroxylamine gave the expected (Z,E)-3-(hydroxyimino)-2-(arylethynyl)furocoumarins with an (Z:E) ratio of about 1:0...
May 31, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28545385/effect-on-acetylcholinesterase-and-anti-oxidant-activity-of-synthetic-chalcones-having-a-good-predicted-pharmacokinetic-profile
#4
Renata Parruca Sakata, Micheli Figueiro, Daniel Fabio Kawano, Wanda Pereira Almeida
BACKGROUND: Acetylcholinesterase (AChE) is an important target in the development of drug to treat Alzheimer´s disease (AD). In this work, we investigated the effect of twenty-two synthesized chalcones on AChE activity. OBJECTIVE: This work is aimed to synthesize and evaluate the effect of chalcones on the AChE activity, as well as anti-oxidant activity and predict their pharmacokinetic profile. METHODS: Chalcones were synthesized through a Claisen-Schmidt condensation and their inhibitory effect on the AChE was evaluated by Elmann's colorimetric method...
May 25, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28545384/synthesis-and-analgesic-activity-of-amines-combining-diazaadamantane-and-monoterpene-fragments
#5
Konstantin Ponomarev, Ekaterina Morozova, Alla Pavlova, Evgeniy Suslov, Dina Korchagina, Andrej Nefedov, Tat Yana Tolstikova, Konstantin Volcho, Nariman Salakhutdinov
BACKGROUND: It was found earlier that compounds combining diazaadamantane and monoterpene moieties possessed promising analgesic activity along with low acute toxicity and the lack of ulcerogenic activity. OBJECTIVE: In this paper, new structural analogues of the most active compounds were synthesized and evaluated for their analgesic activity. METHODS: Their structures were confirmed by various analytical methods, such as 1H and 13C NMR, HRMS...
May 25, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28545383/quinolinic-carboxylic-acid-derivatives-as-potential-multi-target-compounds-for-neurodegeneration-monoamine-oxidase-and-cholinesterase-inhibition
#6
Nehal Afreen Khan, Imtiaz Khan, Syed Mobasher Ali Abid, Sumera Zaib, Aliya Ibrar, Hina Andleeb, Shahid Hameed, Jamshed Iqbal
BACKGROUND: Parkinson's disease (PD), a debilitating and progressive disorder, is among the most challenging and devastating neurodegenerative diseases predominantly affecting the people over 60 years of age. OBJECTIVES: To confront PD, an advanced and operational strategy is to design single chemical functionality able to control more than one target instantaneously. METHODS: In this endeavor, for the exploration of new and efficient inhibitors of Parkinson's disease, we synthesized a series of quinoline carboxylic acids (3a‒j) and evaluated their in-vitro monoamine oxidase and cholinesterase inhibitory activities...
May 25, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28530547/application-of-machine-learning-approaches-for-protein-protein-interactions-prediction
#7
Mengying Zhang, Qiang Su, Yi Lu, Manman Zhao, Bing Niu
BACKGROUND: Proteomics endeavors to study the structures, functions and interactions of proteins. Information of the protein-protein interactions (PPIs) helps to improve our knowledge of the functions and the 3D structures of proteins. Thus determining the PPIs is essential for the study of the proteomics. OBJECTIVE: In this review, in order to study the application of machine learning in predicting PPI, some machine learning approaches such as support vector machine (SVM), artificial neural networks (ANNs) and random forest (RF) were selected, and the examples of its applications in PPIs were listed...
May 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28530546/the-role-of-qsar-and-virtual-screening-studies-in-type-2-diabetes-drug-discovery
#8
Simone Q Pantaleão, Drielli G V Fujji, Vinícius G Maltarollo, Danielle da C Silva, Gustavo H G Trossini, Karen C Weber, Luis P B Scott, Kathia M Honorio
BACKGROUND: Due to the increasing number of diabetes cases worldwide, there is an international concern to provide even more effective treatments to control this condition. METHODS: This review brings together a selection of studies that helped to broaden the comprehension of various biological targets and associated mechanisms involved in type 2 diabetes mellitus. RESULTS: Such studies demonstrated that QSAR techniques and virtual screenings have been successfully employed in drug design projects...
May 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28530545/synthesis-and-biological-evaluation-of-curcumin-nitroxide-based-molecular-hybrids-as-antioxidant-and-anti-proliferative-agents
#9
Balázs Bognár, Muthulakshmi Kuppusamy, Esha Madan, Tamás Kálai, Mária Balog, József Jekő, Periannan Kuppusamy, Kálmán Hideg
BACKGROUND: Natural products and their derivatives are widely used to treat cancer and other diseases associated with ROS- and RNS-induced damages. METHODS: A series of paramagnetic modified curcumin analogues and 3,5-diarylidene-piperidones (DAP) have been designed, synthesized, and characterized on their anti-proliferative and antioxidant activity. RESULTS: Biological characterization of the new compounds supported the earlier results that incorporation of a nitroxide moiety or its precursor into curcumin or diarylidenylpiperidone (DAP) scaffolds resulted in anti-proliferative effect toward cancerous cell-lines in case of aryl hydroxy and/or methoxy substituent containing derivatives suggesting their potential for targeted therapeutic applications...
May 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28523998/uncovering-drug-mechanism-of-action-by-proteome-wide-identification-of-drug-binding-proteins
#10
Tao Cui, Hai Hou, Yao Sun, Huaixing Cang, Xiangxi Wang
Small molecule drugs obtained from synthetic compounds or natural products show their therapeutic effects by specifically binding to one or a few target proteins and modulating their functions. In contrast, undesirable drug-protein interactions may provoke harmful side effects. Furthermore, drug-protein interactions also play roles in drug activation, transport, metabolism and regulation of drug resistance. Therefore, systematically identifying binding proteins of a drug molecule is critical for understanding the mechanism of action of the drug at molecular level...
May 18, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28521678/ipgk-pseaac-identify-lysine-phosphoglycerylation-sites-in-proteins-by-incorporating-four-different-tiers-of-amino-acid-pairwise-coupling-information-into-the-general-pseaac
#11
Li-Ming Liu, Yan Xu, Kuo-Chen Chou
BACKGROUND: Occurring at Lys residues, the PGK (lysine phosphoglycerylation) is a special kind of post-translational modification (PTM). It may invert the charge potential of the modified residue and change the protein structures and functions, causing various diseases in liver, brain, and kidney. OBJECTIVE: From the angles of both basic research and drug development, we are facing a critical challenging problem: for an uncharacterized protein sequence containing many Lys residues, which ones can be of phosphoglycerylation, and which ones cannot? METHOD: To address this problem, we have developed a predictor called iPGK-PseAAC by incorporating into the general PseAAC (pseudo amino acid composition) with four different tiers of amino acid pairwise coupling information, where tiers 1, 2, 3, and 4 refer to the amino acid pairwise couplings between all the 1st, 2nd, 3rd, and 4th most contiguous residues along a protein segment, respectively...
May 15, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28494727/expression-of-toll-like-receptor-2-and-toll-like-receptor-4-in-tuberculous-pleural-effusion
#12
Ying-Zhong Lin, Ting-Mei Feng, Jiao Lan, Chun-Xia Chen, Zhi-Qiang Qin, Yan-Bin Wu, Huan-Zhong Shi, Jian-Bo Ye, Cai-Zhou Wei, Wu Wang, Lu-Ying Huang
BACKGROUND: Toll-like receptor-2 (TLR2) and Toll-like receptor-4 (TLR4) have been reported to play a crucial role in tuberculosis, however, little is known about their expression in tuberculous pleuritis. OBJECTIVE: The goal of this work is to explore the expressions of TLR2 and TLR4 in tuberculous pleuritis and their predominant expressions on cells. METHODS: Levels of soluble TLR2 and TLR4 by enzyme linked immunosorbent assay (ELISA) in 58 patients with tuberculous pleural effusion (PE) and 43 with malignant PE were determined...
May 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28494726/chlorella-vulgaris-induces-apoptosis-of-human-non-small-cell-lung-carcinoma-nsclc-cells
#13
Zhi-Dong Zhang, Kai Liang, Kun Li, Guo-Quan Wang, Ke-Wei Zhang, Lei Cai, Shui-Ting Zhai, Kuo-Chen Chou
PURPOSE: Chlorella vulgaris(C. vulgaris), a unicellular green microalga, has been widely used as a food supplement and reported to have antioxidant and anticancer properties. The current study was designed to assess the cytotoxic, apoptotic, and DNA-damaging effects of C. vulgaris growth factor (CGF), hot water C. vulgaris extracts, in lung tumor A549 and NCI-H460 cell lines. METHODS: A549 cells, NCI-H460 cells, and normal human fibroblasts were treated with CGF at various concentrations (0-300 μg/ml) for 24 hr...
May 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28494725/computational-methods-for-predicting-ncrna-protein-interactions
#14
Shao-Wu Zhang, Xiao-Nan Fan
BACKGROUND: RNA-protein interactions (RPIs) play an important role in many cellular processes. In particular, noncoding RNA-protein interactions (ncRPIs) are involved in various gene regulations and human complex diseases. High-throughput experiments have provided a large number of valuable information about ncRPIs, but these experiments are expensive and time-consuming. Therefore, some computational approaches have been developed to predict ncRPIs efficiently and effectively. METHODS: In this work, we will describe the recent advance of predicting ncRPIs from the following aspects: i) the dataset construction; ii) the sequence and structural feature representation, and iii) the machine learning algorithm...
May 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28494724/c-type-lectin-receptor-old-friend-and-new-player
#15
Hai Hou, Yahui Guo, Qing Chang, Tianming Luo, Xin Wu, Xueqiang Zhao
During the last two decades, C-type lectin receptors (CLRs) have been demonstrated to play key roles in initiating the host immune response upon fungal infection. It is well established that CLRs, such as Dectin-1, Dectin-2, Dectin-3 and Mincle, recognize the cell wall component from the infected microorganisms by using their carbohydrate recognition domain (CRD). Upon stimulation, CLRs induce multiple signal transduction cascades through their own immune-receptor tyrosine-based activation motifs (ITAMs) or interacting with ITAM-containing adaptor proteins such as FcRγ, which then lead to the activation of nuclear factor kappa B (NF-kB) through Syk- and CARD9-dependent pathway...
May 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28480832/synthesis-of-new-arylidene-2-5-diketopiperazines-and-evaluation-of-their-anti-acetylcholinesterase-anti-xanthine-oxidase-anti-diabetic-and-cytotoxic-activities
#16
Mohamed Amine Belkacem, Hichem Ben Jannet, Hicham Ferhout, Laila Mzali, Jalloul Bouajila
BACKGROUND: 2,5-diketopiperazine derivatives are considered to be important classes of cyclic peptides due to their wide range of biological activities. OBJECTIVES: Synthesis a new series of protected 2,5-diketopiperazine derivatives and evaluate their biological activities. METHODS: A series of new soluble mono-protected arylidene 2,5-diketopiperazine derivatives 3a-p has been prepared by application of Claisen-Schmidt condensation of the N,N-diacetyl-diketopiperazine 1 with a series of arylaldehydes...
April 25, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28440189/better-predictive-value-of-cancer-antigen125-ca125-as-biomarker-in-ovary-and-breast-tumors-and-its-correlation-with-the-histopathological-type-grade-of-the-disease
#17
Aarifa Nazmeen, Smarajit Maiti, Kusumita Mandal, Samir K Roy, Tamal Kanti Ghosh, Nirmalya K Sinha, Kamalika Mandal
BACKGROUND: Both ovarian/breast cancers are the most prevalent hormone-associated gynecological-cancers, where uncontrolled cellular proliferations/genetic-errors are noticed. The cancer-antigen125 (CA125), which we assessed presently is an important biomarker in the early detection/monitoring of this disease-pathogenesis. METHODS: Serum/tissue CA125 was measured by solid-phase-Enzyme-linked-immunosorbent-assay in women with ovarian/breast tumors of different types (epithelial/non-epithelial; benign/borderline/malignant)/stages...
April 24, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28427245/the-impact-of-dids-induced-inhibition-of-voltage-dependent-anion-channels-vdac-on-cellular-response-of-lymphoblastoid-cells-to-ionizing-radiation
#18
Magdalena Skonieczna, Artur Cieślar-Pobuda, Yuriy Saenko, Marek Foksiński, Ryszard Oliński, Joanna Rzeszowska-Wolny, Emilia Wiechec
Background: The voltage-dependent ion channels (VDAC) play an essential role in the cross talk between mitochondria and the rest of the cell. Their implication in cell life and cell death has been studied extensively in recent years. In this work we studied the impact of mitochondrial membrane voltage-dependent anion channels (VDACs) on cell survival and response to X-ionizing radiation (IR) of human lymphoblastoid K562 cells. Methods: The inhibition of VDACs was achieved by 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid (DIDS) inhibitor and in vitro experiments including clonogenity assay, UV-visible spectrophotometry, comet assay and FACS analysis were implemented...
April 21, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28425870/ipreny-pseaac-identify-c-terminal-cysteine-prenylation-sites-in-proteins-by-incorporating-two-tiers-of-sequence-couplings-into-pseaac
#19
Yan Xu, Zu Wang, Chunhui Li, Kuo-Chen Chou
PURPOSE: Occurring at the cysteine residue in the C-terminal of a protein, prenylation is a special kind of post-translational modification (PTM), which may play a key role for statin in altering immune function. Therefore, knowledge of the prenylation sites in proteins is important for drug development as well as for in-depth understanding the biological process concerned. Given a query protein whose C-terminal contains some cysteine residues, which one can be of prenylation or none of them can be prenylated? METHODS: To address this problem, we have developed a new predictor, called "iPreny-PseAAC", by incorporating two tiers of sequence pair coupling effects into the general form of PseAAC (pseudo amino acid composition)...
April 19, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28359234/identification-of-novel-5-6-dimethoxyindan-1-one-derivatives-as-antiviral-agents
#20
Siddappa A Patil, Vikrant Patil, Renukadevi Patil, Kenneth Beaman, Shivaputra A Patil
BACKGROUND: Discovery of novel antiviral agents is essential because viral infection continues to threaten human life globally. Various heterocyclic small molecules have been developed as antiviral agents. The 5,6-dimethoxy indan-1-one nucleus is of considerable interest as this ring is the key constituent in a range of bioactive compounds, both naturally occurring and synthetic, and often of considerable complexity. OBJECTIVE: The main purpose of this research was to discover and develop small molecule heterocycles as broad-spectrum of antiviral agents...
March 29, 2017: Medicinal Chemistry
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