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Call For Paper
Bentham Science Publishers would like to invite you to submit your research paper for publishing in the Journal of
Thursday, November 3, 2016
Highlighted Artcile: The Disulfide Analogues of Isophosphoramide Mustard for Anticancer Therapy
The Disulfide Analogues of Isophosphoramide Mustard for Anticancer Therapy
Author(s):
Joanna Cytarska, Krzysztof Skowerski, Szymon Jaworski, Konrad Misiura, Beata Filip-Psurska and Joanna Wietrzyk Pages 172 - 179 ( 8 )
Abstract:
Novel disulfide analogues of isophosphoramide mustard (iPAM) were designed and synthesised. All compounds were hydrolytically stable and underwent reduction by L-glutathione with different kinetic parameters. Based on the HPLC-MS analysis a mechanism of activation by glutathione obtained disulfide analogues of iPAM was proposed. The compounds were tested for cytotoxic activity against human promyelocytic leukaemia HL-60, human lymphoblastic leukaemia MOLT-4, human lymphoblastic leukaemia CCRF/CEM, human bladder cancer HCV29T, murine melanoma B16-F0 and murine fibroblasts Balb3T3 cell lines. The most promising anticancer activity was exhibited by compound 4, which proved to be more active than the reference cisplatin against all cancer cell lines.
Keywords:
Anticancer activity, disulfide, glutathione, isophosphoramide mustard.
Affiliation:
Department of Chemical Technology and Pharmaceuticals, Faculty of Pharmacy, Collegium Medicum, Nicolaus Copernicus University, Jurasza 2, 85-089 Bydgoszcz, Poland.
Graphical Abstract:
For More Information Please Visit Our Website Current Letter in Drug Design & Discovery
Thursday, October 27, 2016
Most Cited Article: In Silico, Spectroscopic, and Biological Insights on Annelated Pyrrolo[3,2- e]Pyrimidines with Antiproliferative Activity
In Silico, Spectroscopic, and Biological Insights on Annelated
Pyrrolo[3,2- e]Pyrimidines with Antiproliferative Activity
Author(s):
Antonino Lauria, Alessio Terenzi, Carla
Gentile, Annamaria Martorana, Giuseppe Gennaro, Giampaolo Barone and Anna Maria
Almerico Pages 15 - 26 ( 12 )
Abstract:
The in silico COMPARE analysis was performed
on 8-[3-(piperidino)propyl]-4,10-dimethyl-9-phenyl-6-
(methylsulfanyl)-3,4-dihydropyrimido[1,2-c]pyrrolo[3,2-e]pyrimidin-2(8H)-one, a
compound with promising antiproliferative activity, previously synthetized and
screened against a panel of 60 human tumor cell lines. The results evidenced
that this compound matches the biological properties of Chromomycin A3 and
Actinomycin D, known drugs with high DNA binding affinity. Prompted by such
results, a thorough spectroscopic investigation of its DNA aqueous solutions
was performed, with the aim to verify its DNA-binding properties. DNA
groove-binding interaction was assigned by UV-vis spectrophotometric and
circular dichroism (CD) titrations. In agreement with the spectroscopic
studies, the test compound has achieved significant cell-cycle perturbation
with higher accumulation of cells in G0/G1 phase. Further structure
modifications of the tested compound, has led to its analogue, which showed DNA
base-pairs intercalating ability. Molecular modeling studies on the annelated pyrrolo[3,2-e]pyrimidines
tested were in agreement with the biological evaluation.
Keywords:
Anticancer drugs, DNA interactive drugs,
COMPARE analysis, Annelated pyrrolo-pyrimidines, UV-vis DNA titrations,
Circular Dichroism, Ethidium bromide displacement assay, Cell Cycle.
Affiliation:
Via Archirafi 32, 90123 Palermo – Italy.
For More Information Please Visit Our Website Letter in Drug Design Discovery
Thursday, October 20, 2016
Thursday, October 13, 2016
Letters in Drug Design & Discovery, Volume 13 - Number 9
Contents
Letters in Drug Design & Discovery, Volume 13 - Number 9
Structure-based Drugs Design Studies on Spleen Tyrosine Kinase Inhibitors
, 13(9): 845 - 858Letícia Cristina Assis, Letícia Santos Garcia, Daiana Teixeira Mancini, Tamiris Maria Assis, Daniela Rodrigues Silva, Giovanna Gajo Cardoso, Alexandre Alves de Castro, Teodorico Castro Ramalho and Elaine Fontes Ferreira da Cunha.
DOI: 10.2174/1570180813666160725095118
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In-silico Designing of Novel Camptothecin Analogues as Potent Inhibitors of Topoisomerase I: A Molecular Docking, QSAR, and ADME-T Study
, 13(9): 859 - 868Darpan Raghav, Babukrishna Maniyadath, Aruna Mohan, Sutari Sairam, Rinu Mary Rajan and Krishnan Rathinasamy.
DOI: 10.2174/1570180813666160518123550
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Synthesis, Biological Evaluation and in silico Studies of Novel 5α-aza-Bhomo-3,5-secosteroids as Potential 5-reductase Inhibitors
, 13(9): 869 - 878Rajnish Kumar, Pankaj Chauhan, Priyanka Malla, Manoj K. Mahapatra, Rolf W. Hartmann, Jörg Haupenthal and Manoj Kumar.
DOI: 10.2174/1570180813666160630110649
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Identification of Novel IRAK-4 Inhibitors Through Pharmacophore Modeling, Atom-based 3D-QSAR, Docking Strategies and Molecular Dynamics Simulation
,13(9): 879 - 887Liangliang Zhong, Lu Zhou, Yahui Tian and Rong You.
DOI: 10.2174/1570180813666160421163027
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Imidazole-based Derivatives as Potential Anti-platelet Inhibitors: DFT and Molecular Docking Study
, 13(9): 888 - 896Mehbub I. K. Momin, Neil A. Koorbanally and Bahareh Honarparvar.
DOI: 10.2174/1570180813666160517162937
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Synthesis and Antiacetylcholinesterase Activity Evaluation of New 2-aryl Benzofuran Derivatives
, 13(9): 897 - 902Behjat Pouramiri, Mohammad Mahdavi, Setareh Moghimi, Loghman Firoozpour, Hamid Nadri, Alireza Moradi, Esmat Tavakolinejad-Kermani, Ali Asadipourand Alireza Foroumadi.
DOI: 10.2174/1570180813666160610124637
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Synthesis and Evaluation of New Thiazole Derivatives as Potential Antimicrobial Agents
, 13(9): 903 - 911Mehlika Dilek Altıntop, Ahmet Özdemir, Özlem Atlı, Zerrin Cantürk, Merve Baysal and Zafer Asım Kaplancıklı.
DOI: 10.2174/1570180813666160226001021
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Synthesis and In vivo Antifibrotic Activity of Novel Leflunomide Analogues
, 13(9): 912 - 920Abdelrahman Hamdi, Eman Said, Abdelbasset A. Farahat, Serry A. A. El-Bialy and Mohammed A M Massoud.
DOI: 10.2174/1570180813666160630125624
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Synthesis and Antimicrobial Evaluation of New Pyrazoline and Pyrazolinyl Thiazole Derivatives Bearing Tetrazolo[1,5-a]quinoline Moiety
, 13(9): 921 - 931Ibrahim A. M. Radini, Rizk E. Khidre and Emad M El-Telbani.
DOI: 10.2174/1570180813666160712234454
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Design, Synthesis and Antimalarial Activity of Some New Aminoalcoholpyrrolo[1,2-a]quinoxaline Derivatives
, 13(9): 932 - 942Jean Guillon, Stéphane Moreau, Luisa Ronga, Louise Basmacyian, Anita Cohen, Sandra Rubio, Guillaume Bentzinger, Solène Savrimoutou, Nadine Azas,Catherine Mullié and Pascal Sonnet.
DOI: 10.2174/1570180813666160517164758
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Significance of Amino Group Substitution at Combretastatin A-4 and Phenstatin Analogs
, 13(9): 943 - 951Vijay K. Patel and Harish Rajak.
DOI: 10.2174/1570180813666160517163444
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Study of Some Piperine Analogues on Drugs Efflux by Targeting P-glycoprotein, an in silico Approach
, 13(9): 952 - 961Anushree Tripathi, Krishna Misra and Rajesh Kumar Kesharwani.
DOI: 10.2174/1570180813999160830102312
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Sodium Channel Blocking Activity and In-vivo Testing of New Phenylimidazole Derivatives
, 13(9): 962 - 967Mirko Rivara, Manoj K. Patel, Alberto Rapalli and Valentina Zuliani.
DOI: 10.2174/1570180813666160714125755
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An Efficient Nonconventional Glycerol-Based Solid Acid Catalyzed Synthesis and Biological Evaluation of Phosphonate Conjugates of 1,2,4-triazole Thiones
,13(9): 968 - 981Madugula S. R. Murty, Mohana R. Katiki, Busam R. Rao, Sai S. Narayanan, Ruby J. Anto, Sudhreer K. Buddana, Reddy S. Prakasham, Bethala L. A. P. Devi andRachapudi B N Prasad.
DOI: 10.2174/1570180813666160125222334
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Design, Synthesis and Molecular Docking Studies of 2-Aryl/Heteroaryl-Ethyl 6-Chloroquinoline-4-Carboxylates as Potential Antimalarial Agents
, 13(9): 982 - 991Thamatakallu O. S. Kumar, Kittappa M. Mahadevan, Pasura S. Sujanganapathy and Manikyanahally N Kumara.
DOI: 10.2174/1570180813666160722112725
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