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Antioxidant Activity of Synthetic Resveratrol Analogs: A Structure-Activity Insight
Natalia Oliveira Calil,Gustavo Senra Gonçalves de Carvalho, Annelisa Farah da Silva, Adilson David da Silva and Nádia Rezende Barbosa Raposo
[Abstract] [FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00261]
Novel Aminoalcohol Derivatives Bearing 4-Phenylphenol as Antischistosomal Drugs
Li-Ping Duan, Jian Xue, Yi Tao and Hao-Bing Zhang
[Abstract] [FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00262]
Quantitative Structural Activity Relationship Studies for NSAIDs as chemopreventive agents in Colon Cancer Cell Lines using Self Organizing Molecular Field Analysis
Honey Goel, Suresh Thareja, Priyanka Malla, Manoj Kumar and V. R Sinha
[Abstract] [FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00263]
In Vitro Activity Against Trypanosoma cruzi and Leishmania chagasi Parasites of 2,4-Diaryl 1,2,3,4-Tetrahydroquinoline Derivatives
Arnold R. Romero Bohórquez, Patricia Escobar Rivero, Sandra M. Leal and Vladimir V. Kouznetsov
[Abstract] [FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00264]
Quantitative Measurement of Some Physico-Chemical Parameters for the Medicinally Useful Natural Products
Sethi, Koyel Kar, D. Archana, S. Vasavi, P. Maheswari, P. Niranjini, L. Vimalacharitha, W. Prathyusha, V. Sai Thanuja, K. Sreejana Reddy, G. Rohith, Amnish Kumar, A. G. Damodar and B. R. Prashantha Kumar
[Abstract] [FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00265]
Synthesis and biological evaluation of novel 4-indolyl-5-phenyl (indolyl)-1,2-dihydropyrazol-3-ones as glycogen synthase kinase-3β (GSK-3β) inhibitors
Hong Yin, Fengying Sui, Xinji Yang, Yingying Shangguan and Guojie Song
[Abstract] [FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00266]
Abstracts
Antioxidant Activity of Synthetic Resveratrol Analogs: A Structure-Activity Insight
Natalia Oliveira Calil,Gustavo Senra Gonçalves de Carvalho, Annelisa Farah da Silva, Adilson David da Silva and Nádia Rezende Barbosa Raposo
[Abstract] [FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00261]
This study evaluated the antioxidant activity of five resveratrol analogs using the DPPH method. The molecules activity was related with their chemical structure. Besides descriptive statistics, the analysis of variance (ANOVA) followed by Tukey’s post hoc test were performed (p<0.05). The antioxidant activity of analogs A and B was statistically similar from each other and from the reference standard resveratrol, possibly due to the presence of 4-hydroxy grouping. The aromatic hydroxyl reduces reactive free radicals and produces phenoxyl radical, stabilized by resonance. Although the analog C has shown IC50 value statistically different from the resveratrol (p<0.001), its antioxidant activity was considered satisfactory. The other analogues (D and E), which have a 4-acid grouping in place of 4-hydroxy grouping, showed lower antioxidant activity than resveratrol (p<0.001). Further studies to address possible advantages of analogs in relation to resveratrol should be conducted in order to make them feasible for therapeutic use.
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Novel Aminoalcohol Derivatives Bearing 4-Phenylphenol as Antischistosomal Drugs
Li-Ping Duan, Jian Xue, Yi Tao and Hao-Bing Zhang
[FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00262]
There is a need to develop new antischistosomal compounds when the only available therapeutic agents praziquantel large-scale used in the world. A series of novel aminoalcohol derivatives bearing 4-phenylphenol moiety were designed and synthesized. The structures of all the newly synthesized compounds were identified by elemental analysis, 1H-NMR, 13C-NMR and LC-MS. Their biological activities were evaluated against Schistosoma japonicum in mice by an oral route. Among these compounds, in vivo, at concentrations of 400mg/kg of mouse, compound 1-(biphenyl-4’-yloxy)-3-(1’-(3’,4’-difluorophenyl)ethylamino)propan-2-ol (3j) produced the highest activity with 93.0% deparasitization. These compounds may find usefulness in the discovery and development of new antischistosomal drugs.
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Quantitative Structural Activity Relationship Studies for NSAIDs as chemopreventive agents in Colon Cancer Cell Lines using Self Organizing Molecular Field Analysis
Honey Goel, Suresh Thareja, Priyanka Malla, Manoj Kumar and V. R Sinha
[FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00263]
Non-steroidal anti-inflammatory drugs (NSAIDs) have emerged as promising agents to accelerate the future clinical management of colon cancer chemoprevention. NSAIDs exhibit a vital role as mono as well as combination therapy with conventional anticancer drugs for the prophylaxis and management of various cancers, including colon carcinogenesis. In vitro cell-based cytotoxicity assays are effective techniques for hit ranking and lead optimization at the early stage of drug discovery. The present study has been focused on in silico screening and prediction of in vitro cytotoxicity (or growth inhibitory activity, GI50) of heterogeneous group of NSAIDs having flexibility in structure and cytotoxicity activity against DLD-1 and SW-480 colon cancer cell lines using 3D-QSAR (3-dimensional quantitative structural activity relationship) SOMFA (self-organizing molecular field analysis) studies. The statistically validated robust models were obtained using SOMFA having good cross-validated correlation coefficients of r2cv (0.5649 and 0.5049), non-cross validated correlation coefficient r2 values (0.6887 and 0.6465) and high F-test value (14.01 and 11.58) for both DLD-1 cell lines and SW-480 cell lines respectively. Analysis of 3D-QSAR models through electrostatic and shape grids provide useful information about the steric, electrostatic potential contributions along with the combination of log P, total dipole moment and molar refractivity (MR) on GI50. The results obtained provided an insight on NSAIDs with optimum in vitro cytotoxicity activity and improved therapeutic profile.
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In Vitro Activity Against Trypanosoma cruzi and Leishmania chagasi Parasites of 2,4-Diaryl 1,2,3,4-Tetrahydroquinoline Derivatives
Arnold R. Romero Bohórquez, Patricia Escobar Rivero, Sandra M. Leal and Vladimir V. Kouznetsov
[FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00264]
Diverse polyfunctionalized tetrahydroquinolines, easily prepared using BF3.OEt2-catalyzed three component imino Diels–Alder reaction, were tested in vitro against Trypanosoma cruzi and Leishmania chagasi parasites and also for cytotoxicity using Vero and THP-1 mammalian cell lines. These studies showed that the most active compound was 7h (IC50 5.77 ± 0.21; IC90 40.43 ± 1.58 μM for T. cruzi and IC50 0.27 ± 0.03; IC90 2.16± 0.37 μM for L. chagasi) has selective index (SI) values greater than the reference drugs (SI > 46 and SI > 1000 in epimastigotes form of T. cruzi and promastigotes form of L. chagasi parasites, respectively). Moreover, the comp. 7h did not show cytotoxicity against Vero or THP-1 cells (IC50 > 270 μM).
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Quantitative Measurement of Some Physico-Chemical Parameters for the Medicinally Useful Natural Products
Sethi, Koyel Kar, D. Archana, S. Vasavi, P. Maheswari, P. Niranjini, L. Vimalacharitha, W. Prathyusha, V. Sai Thanuja, K. Sreejana Reddy, G. Rohith, Amnish Kumar, A. G. Damodar and B. R. Prashantha Kumar
[FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00265]
Lipinski’s rule of five is well received throughout the world and widely used as one of the basic filters to screening ligands for their druggability. In this direction, we have studied on 150 biologically active natural products which are available as drugs. Physicochemical parameters such as molecular weight, logP, hydrogen bond donors, hydrogen bond acceptors, number of aromatic rings, molar refr and Gibbs free energy were calculated. Statistical results reveal that, they do fall under the Lipinski’s rule of 5 (RO5). The illustration about need for the study, methods followed and results obtained are reported here.
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Synthesis and biological evaluation of novel 4-indolyl-5-phenyl (indolyl)-1,2-dihydropyrazol-3-ones as glycogen synthase kinase-3β (GSK-3β) inhibitors
Hong Yin, Fengying Sui, Xinji Yang, Yingying Shangguan and Guojie Song
[FULL-TEXT INQUIRY] [BSP/LDDD/E-Pub/00266]
A novel series of 4-indolyl-5-phenyl (indolyl)-1,2-dihydropyrazol-3-ones were synthesized and evaluated for their GSK-3β inhibitory activity. Half of the tested compounds showed moderate GSK-3β inhibitory activity. Preliminary structure-activity relationships were discussed and showed that substituents on the benzene ring and N1-position of the indole ring have a significant effect on the potency. Compounds 11c and 14, the most potent ones with IC50 values of 9.28 and 8.98 μM respectively, would be promising templates for further development of novel GSK-3β inhibitors.
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