Thursday, December 22, 2016

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Thursday, November 24, 2016

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Thursday, November 10, 2016

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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.

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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.



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Thursday, October 20, 2016

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Thursday, October 13, 2016

Letters in Drug Design & Discovery, Volume 13 - Number 9


Contents

Letters in Drug Design & DiscoveryVolume 13 - Number 9

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