1,738 results match your criteria Future Medicinal Chemistry [Journal]


From the magic bullet to the magic target: exploiting the diverse roles of DDX3X in viral infections and tumorigenesis.

Future Med Chem 2019 Feb 28. Epub 2019 Feb 28.

Department of DNA Enzymology & Molecular Virology, Institute of Molecular Genetics IGM-CNR, via Abbiategrasso 207, I-27100 Pavia, Italy.

DDX3X is an ATPase/RNA helicase of the DEAD-box family and one of the most multifaceted helicases known up to date, acting in RNA metabolism, cell cycle control, apoptosis, stress response and innate immunity. Depending on the virus or the viral cycle stage, DDX3X can act either in a proviral fashion or as an antiviral factor. Similarly, in different cancer types, it can act either as an oncogene or a tumor-suppressor gene. Read More

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http://dx.doi.org/10.4155/fmc-2018-0451DOI Listing
February 2019

The advantages and challenges raised by the chemistry of aldehydic cellulose nanofibers in medicinal chemistry.

Future Med Chem 2018 Dec;10(23):2679-2683

University Grenoble Alpes, DPM, CNRS, F-38000 Grenoble, France.

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http://dx.doi.org/10.4155/fmc-2018-0277DOI Listing
December 2018
1 Read

How to replace the lost keys? Strategies toward safer K7 channel openers.

Future Med Chem 2019 Feb 25. Epub 2019 Feb 25.

Pharmaceutical & Medicinal Chemistry, Institute of Pharmacy, University of Greifswald, Friedrich-Ludwig-Jahn-Str. 17, 17487 Greifswald, Germany.

The highly structurally similar drugs flupirtine and retigabine have been regarded as safe and effective for many years but lately they turned out to exert intolerable side effects. While the twin molecules share the mode of action, both stabilize the open state of voltage-gated potassium channels, the form and severity of adverse effects is different. The analgesic flupirtine caused drug-induced liver injury in rare but fatal cases, whereas prolonged use of the antiepileptic retigabine led to blue tissue discoloration. Read More

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http://dx.doi.org/10.4155/fmc-2018-0350DOI Listing
February 2019

Gaseous signaling molecules and their application in resistant cancer treatment: from invisible to visible.

Future Med Chem 2019 Feb 25. Epub 2019 Feb 25.

Department of Pharmaceutical Sciences, College of Pharmacy & Health Sciences, St John's University, Queens, NY 11439, USA.

Multidrug resistance (MDR) in cancer remains a critical obstacle for efficient chemotherapy. Many MDR reversal agents have been discovered but failed in clinical trials due to severe toxic effects. Gaseous signaling molecules (GSMs), such as oxygen, nitric oxide, hydrogen sulfide and carbon monoxide, play key roles in regulating cell biological function and MDR. Read More

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http://dx.doi.org/10.4155/fmc-2018-0403DOI Listing
February 2019

Hydroxylation of protein constituents of the human translation system: structural aspects and functional assignments.

Future Med Chem 2019 Feb 25. Epub 2019 Feb 25.

Institute of Chemical Biology & Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences, pr. Lavrentieva, 8, 630090 Novosibirsk, Russia.

During the current decade, data on the post-translational hydroxylation of specific amino acid residues of some ribosomal proteins and translation factors in both eukaryotes and eubacteria have accumulated. The reaction is catalyzed by dedicated oxygenases (so-called ribosomal oxygenases), whose action is impaired under hypoxia conditions. The modification occurs at amino acid residues directly involved in the formation of the main functional sites of ribosomes and factors. Read More

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http://dx.doi.org/10.4155/fmc-2018-0317DOI Listing
February 2019

Improving the accuracy of predicting protein-ligand binding-free energy with semiempirical quantum chemistry charge.

Future Med Chem 2019 Feb 25. Epub 2019 Feb 25.

Drug Discovery & Design Center, CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai, 201203, PR China.

Aim: It is a challenge to predict binding-free energy (ΔG) accurately.

Methodology/results: For accurate ΔG prediction, a new strategy combining solvated interaction energy (SIE) or molecular mechanics/generalized Born surface area (MM/GBSA) approach with the Coulson charge of both protein and ligand calculated by semiempirical quantum mechanics (SQM), named SIE-SQMPC or MM/GBSA-SQMPC approach, was developed and tested on 50 protein-ligand complexes. Both approaches achieved higher correlation (R ) between experimental and predicted ΔG than that with Amber-ff03 charge, even for ligands with highly different scaffolds. Read More

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http://dx.doi.org/10.4155/fmc-2018-0207DOI Listing
February 2019

Discovery of new phthalazinones as vasodilator agents and novel pharmacological tools to study calcium channels.

Future Med Chem 2019 Feb 25. Epub 2019 Feb 25.

Departamento de Farmacología, Facultad de Farmacia, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain.

Aim: Hydralazine has led to the synthesis of phthalazinone derivatives which induce vasorelaxation.

Methods: A new series of 2-(aminoalkyl)-4-benzyl-2H-phthalazin-1-one derivatives has been synthesized to study their vasorelaxant activity.

Results: At the highest-studied concentration, most of the new compounds relaxed the denuded aortic rings precontracted with phenylephrine by 72. Read More

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http://dx.doi.org/10.4155/fmc-2018-0250DOI Listing
February 2019
1 Read

Membrane-targeting antibiotics: recent developments outside the peptide space.

Future Med Chem 2019 Feb 25. Epub 2019 Feb 25.

Centro de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, Lisboa, Portugal.

The rise of antibiotic resistant bacteria requires unconventional strategies toward efficient chemotherapeutic agents, preferably with alternative mechanisms of action. The bacterial cell membrane has become an appealing target since its essential and highly conservative structure are key challenges to resistance mechanisms. Inspired by natural antimicrobial peptides, research on membrane-targeting antimicrobials has been growing out of the peptide space. Read More

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http://dx.doi.org/10.4155/fmc-2018-0254DOI Listing
February 2019

GABA receptor family: overview on structural characterization.

Future Med Chem 2019 Feb 25. Epub 2019 Feb 25.

Department of Biotechnology, University of Verona, Strada Le Grazie 15, I-37134 Verona, Italy.

The pentameric γ-aminobutyric acid type A receptors are ion channels activated by ligands, which intervene in the rapid inhibitory transmission in the mammalian CNS. Due to their rich pharmacology and therapeutic potential, it is essential to understand their structure and function thoroughly. This deep characterization was hampered by the lack of experimental structural information for many years. Read More

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http://dx.doi.org/10.4155/fmc-2018-0336DOI Listing
February 2019
1 Read

Benzodifurans for biomedical applications: BZ4, a selective anti-proliferative and anti-amyloid lead compound.

Future Med Chem 2019 Feb 25. Epub 2019 Feb 25.

CNR, Institute of Biostructure & Bioimaging, Via Mezzocannone site & Headquarters, 80134 Naples, Italy.

Aim: Our goal is to evaluate benzodifuran-based scaffolds for biomedical applications.

Methodology: We here explored the anticancer and anti-amyloid activities of a novel compound (BZ4) in comparison with other known benzodifuran analogs, previously studied in our group, and we have explored its ability to interact with different DNA model systems.

Results: BZ4 shows antiproliferative activity on different cancer cells; does not affect noncancerous control cells and alters the aggregation properties of β-amyloid, as ascertained by circular dichroism, fluorescence spectroscopy and scanning electron microscopy analysis. Read More

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http://dx.doi.org/10.4155/fmc-2018-0473DOI Listing
February 2019

Exploring bacterial resistome and resistance dessemination: an approach of whole genome sequencing.

Future Med Chem 2019 Feb 25. Epub 2019 Feb 25.

Medical Microbiology & Molecular Biology, Laboratory Interdisciplinary, Biotechnology Unit, Aligarh Muslim University, Aligarh 202002, India.

For several decades antibiotics are used to combat against pathogenic bacteria, but their misuse and overuse have caused the emergence of resistant bacteria. The scarcities of effective antibiotics along with unavailability of alternative solutions have exacerbated bacterial infections and mortality rate. This review provides the concept of bacterial resistome and mechanisms of resistance. Read More

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http://dx.doi.org/10.4155/fmc-2018-0201DOI Listing
February 2019

Lipophilicity in drug design: an overview of lipophilicity descriptors in 3D-QSAR studies.

Future Med Chem 2019 Feb 25. Epub 2019 Feb 25.

Department of Nutrition, Food Sciences & Gastronomy, Faculty of Pharmacy & Food Sciences, Campus Torribera, Institute of Biomedicine (IBUB), & Institute of Theoretical & Computational Chemistry (IQTC-UB), University of Barcelona, Av. Prat de la Riba 171, Santa Coloma de Gramenet E-08921, Spain.

The pharmacophore concept is a fundamental cornerstone in drug discovery, playing a critical role in determining the success of in silico techniques, such as virtual screening and 3D-QSAR studies. The reliability of these approaches is influenced by the quality of the physicochemical descriptors used to characterize the chemical entities. In this context, a pivotal role is exerted by lipophilicity, which is a major contribution to host-guest interaction and ligand binding affinity. Read More

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http://dx.doi.org/10.4155/fmc-2018-0435DOI Listing
February 2019
1 Read

Synthesis and evaluation of novel 7H-pyrrolo-[2,3-d]pyrimidine derivatives as potential anticancer agents.

Future Med Chem 2019 Feb 21. Epub 2019 Feb 21.

TMU Biomedical Commercialization Center, Taipei Medical University,  Taipei, Taiwan.

Aim: Bladder cancer is a highly recurrent urologic malignancy with limited treatment approaches. Previously, we reported compound 11 is a FGFR3 inhibitor with significant antibladder cancer activity.

Materials & Methods: In this study, a series of 7H-pyrrolo-[2,3-d]pyrimidine derivatives were synthesized through ring formation and modification of compound 11 for anticancer activity evaluation. Read More

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http://dx.doi.org/10.4155/fmc-2018-0564DOI Listing
February 2019

Multitarget-directed ligands for neurodegenerative diseases: real opportunity or blurry mirage?

Future Med Chem 2019 Feb 14. Epub 2019 Feb 14.

Sussex Drug Discovery Centre, School of Life Sciences, University of Sussex, Brighton, BN1 9QJ, UK.

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http://dx.doi.org/10.4155/fmc-2018-0249DOI Listing
February 2019

Designing influenza polymerase acidic endonuclease inhibitors via 'privileged scaffold' re-evolution/refining strategy.

Future Med Chem 2019 Feb 14. Epub 2019 Feb 14.

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, School of Pharmaceutical Sciences, Ministry of Education, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.

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http://dx.doi.org/10.4155/fmc-2018-0489DOI Listing
February 2019

Emerging from the dark side: new therapeutic applications of scheduled psychoactive substances.

Future Med Chem 2019 Feb 14. Epub 2019 Feb 14.

School of Pharmacy & Pharmaceutical Sciences, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, Wales, UK.

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http://dx.doi.org/10.4155/fmc-2018-0447DOI Listing
February 2019

Translating unusual computational methods to drug discovery: taking advantage of work in other fields.

Future Med Chem 2019 Feb 14. Epub 2019 Feb 14.

Molecular Biotechnology & Health Sciences Department, University of Torino, Via Quarello, 15, 10135 Torino, Italy.

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http://dx.doi.org/10.4155/fmc-2018-0287DOI Listing
February 2019

tRNA modification and cancer: potential for therapeutic prevention and intervention.

Future Med Chem 2019 Feb 12. Epub 2019 Feb 12.

Metabolomics Core Resource Laboratory, NYU Langone Health, New York, NY, USA.

Transfer RNAs (tRNAs) undergo extensive chemical modification within cells through the activity of tRNA methyltransferase enzymes (TRMs). Although tRNA modifications are dynamic, how they impact cell behavior after stress and during tumorigenesis is not well understood. This review discusses how tRNA modifications influence the translation of codon-biased transcripts involved in responses to oxidative stress. Read More

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http://dx.doi.org/10.4155/fmc-2018-0404DOI Listing
February 2019
4.000 Impact Factor

Inhibiting two cellular mutant epidermal growth factor receptor tyrosine kinases by addressing computationally assessed crystal ligand pockets.

Future Med Chem 2019 Feb 6. Epub 2019 Feb 6.

Department of Biotechnology, College of Life Science, Kaohsiung Medical University, Kaohsiung, Taiwan.

Aim: Blocking receptor tyrosine kinases is a useful strategy for inhibiting the overexpression of EGFR. However, the quality of crystal pocket is an essential issue for virtually identifying new leads for surviving resistance cancer cells.

Results: With the examinating crystal pocket quality by the self-docking root-mean-square deviation (RMSD) calculation, we used the two best kinase pockets of mutant EGFR kinases, T790M/L858R and G719S, for virtual screening. Read More

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http://dx.doi.org/10.4155/fmc-2018-0525DOI Listing
February 2019

Proteolysis-targeting chimeras for targeting protein for degradation.

Future Med Chem 2019 Feb 1. Epub 2019 Feb 1.

State Key Laboratory of Bioactive Substances & Function of Natural Medicine, Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, PR China.

Proteolysis-targeting chimeras (PROTACs) are an emerging tool for therapeutic intervention by reducing or eliminating disease-causing proteins. PROTACs are bifunctional molecules that consist of a target protein ligand, a linker and an E3 ligase ligand, which mediate the polyubiquitination of the target protein, ultimately leading to the target protein degradation by the ubiquitin-proteasome pathway. We review some of the main PROTACs that have been reported recently and discuss their potential therapeutic benefits over classical enzyme inhibition. Read More

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http://dx.doi.org/10.4155/fmc-2018-0557DOI Listing
February 2019
1 Read
4.000 Impact Factor

Deep learning for molecular generation.

Future Med Chem 2019 Jan 30. Epub 2019 Jan 30.

Center for Quantitative Biology, Academy for Advanced Interdisciplinary Studies, Peking University, Beijing, 100871, PR China.

De novo drug design aims to generate novel chemical compounds with desirable chemical and pharmacological properties from scratch using computer-based methods. Recently, deep generative neural networks have become a very active research frontier in de novo drug discovery, both in theoretical and in experimental evidence, shedding light on a promising new direction of automatic molecular generation and optimization. In this review, we discussed recent development of deep learning models for molecular generation and summarized them as four different generative architectures with four different optimization strategies. Read More

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https://www.future-science.com/doi/10.4155/fmc-2018-0358
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http://dx.doi.org/10.4155/fmc-2018-0358DOI Listing
January 2019
5 Reads

Corrigendum.

Authors:

Future Med Chem 2019 Jan 28;11(2):155. Epub 2019 Jan 28.

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http://dx.doi.org/10.4155/fmc-2018-0206c1DOI Listing
January 2019
1 Read

Alizarin increase glucose uptake through PI3K/Akt signaling and improve alloxan-induced diabetic mice.

Future Med Chem 2019 Jan 16. Epub 2019 Jan 16.

National Center for Research & Development of Edible Fungus Processing Technology, Henan University, Kaifeng 475004, China.

Aim: Alizarin (AZ), that can be isolated from Rubia cordifolia, has biological activities such as antioxidation and anti-inflammatory. This study aimed to investigate the effect of AZ on glucose and lipid metabolism disorders in alloxan-induced diabetic mice and also explored the effect of AZ on insulin resistance in 3T3-L1 adipocytes.

Results: The research showed that AZ could decrease fasting and postprandial blood glucose, TG, TC and MDA, and it could also increase liver glycogen levels and SOD activity in diabetic mice. Read More

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http://dx.doi.org/10.4155/fmc-2018-0515DOI Listing
January 2019
2 Reads

Alpha-carboxynucleoside phosphonates: direct-acting inhibitors of viral DNA polymerases.

Future Med Chem 2019 Jan 16;11(2):137-154. Epub 2019 Jan 16.

Department of Chemistry, Analytical & Biological Chemistry Research Facility, Synthesis & Solid State Pharmaceutical Centre, University College, Cork, Ireland.

Acyclic nucleoside phosphonates represent a well-defined class of clinically used nucleoside analogs. All acyclic nucleoside phosphonates need intracellular phosphorylation before they can bind viral DNA polymerases. Recently, a novel class of alpha-carboxynucleoside phosphonates have been designed to mimic the natural 2'-deoxynucleotide 5'-triphosphate substrates of DNA polymerases. Read More

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https://www.future-science.com/doi/10.4155/fmc-2018-0324
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http://dx.doi.org/10.4155/fmc-2018-0324DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6362432PMC
January 2019
6 Reads

Energy windows for computed compound conformers: covering artefacts or truly large reorganization energies?

Future Med Chem 2019 Jan 16;11(2):97-118. Epub 2019 Jan 16.

Vernalis Research, Department of Chemistry, Granta Park, Great Abington, Cambridge CB21 6GB, UK.

The generation of 3D conformers of small molecules underpins most computational drug discovery. Thus, the conformer quality is critical and depends on their energetics. A key parameter is the empirical conformational energy window (ΔE), since only conformers within ΔE are retained. Read More

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http://dx.doi.org/10.4155/fmc-2018-0400DOI Listing
January 2019
1 Read
4.000 Impact Factor

Gaze through the clinical lens: molecular and clinical advancements of botanicals.

Future Med Chem 2019 Jan 16;11(2):75-77. Epub 2019 Jan 16.

Department of Oncologic Sciences, Mitchell Cancer Institute, University of South Alabama, Mobile, AL 36604, USA.

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http://dx.doi.org/10.4155/fmc-2018-0371DOI Listing
January 2019
1 Read

Experimental free ligand conformations: a missing link in structure-based drug discovery.

Future Med Chem 2019 Jan 16;11(2):79-82. Epub 2019 Jan 16.

Medicinal Chemistry, Oncology, IMED Biotech Unit, AstraZeneca, Cambridge, UK.

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http://dx.doi.org/10.4155/fmc-2018-0339DOI Listing
January 2019
1 Read

Metal-based antitumor compounds: beyond cisplatin.

Future Med Chem 2019 Jan 15;11(2):119-135. Epub 2019 Jan 15.

Metabolic Signalling Group, School of Pharmacy & Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth, Western Australia 6102, Australia.

Despite improvements in the 5-year survival rate to over 80% in cancers, such as Hodgkin lymphoma and testicular cancer, more aggressive tumors including pancreatic and brain cancer still have extremely low survival rates. The establishment of chemoresistance, responsible for the reduction in treatment efficiency and cancer relapse, is one possible explanation for this setback. Metal-based compounds, a class of anticancer drugs, are largely used in the treatment of cancer. Read More

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http://dx.doi.org/10.4155/fmc-2018-0248DOI Listing
January 2019
1 Read

Purine derivatives with heterocyclic moieties and related analogs as new antitumor agents.

Future Med Chem 2019 Jan 15;11(2):83-95. Epub 2019 Jan 15.

Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Universidad de Granada 18071, Spain.

Aim: Identification of new antiproliferative compounds.

Methodology: Four series of compounds were synthesized by the Mitsunobu reaction. Their antiproliferative activity was studied against several cancer cells and a noncancerous fibroblast cell line. Read More

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http://dx.doi.org/10.4155/fmc-2018-0291DOI Listing
January 2019
1 Read

Synthesis, characterization and antidiabetic effects of vanadyl(II) adenosine monophosphate amino acid mixed-ligand complexes.

Future Med Chem 2019 Jan 15. Epub 2019 Jan 15.

Department of Chemistry, College of Science, Princess Nourah bint Abdulrahman University, Riyadh 11671, Saudi Arabia.

Aim: This research paper is aimed at designing a novel insulin alternative for the treatment of diabetes.

Materials & Methods: Six novel vanadyl(II) compounds, [(AMP)(VO)(AA )]·NH, were synthesized from an equimolar ratio of adenosine monophosphate, VOSO and amino acids (AA ).

Results: The magnetic moments and electronic spectra revealed the square pyramidal geometrical structure of the complexes. Read More

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http://dx.doi.org/10.4155/fmc-2018-0471DOI Listing
January 2019
4 Reads
4.000 Impact Factor

NBGNU: a hypoxia-activated tripartite combi-nitrosourea prodrug overcoming AGT-mediated chemoresistance.

Future Med Chem 2018 Dec 18. Epub 2018 Dec 18.

Beijing Key Laboratory of Environmental & Virus Oncology, College of Life Science & Bioengineering, Beijing University of Technology, Beijing 100124, PR China.

Aim: A hypoxia-activated combi-nitrosourea prodrug, N-(2-chloroethyl)-N'-2-(2-(4-nitrobenzylcarbamate)-O -benzyl-9-guanine)ethyl-N-nitrosourea (NBGNU), was synthesized and evaluated for its hypoxic selectivity and anticancer activity in vitro.

Results: The prodrug was designed as a tripartite molecule consisting of a chloroethylnitrosourea pharmacophore to induce DNA interstrand crosslinks (ICLs) and an O -benzylguanine analog moiety masked by a 4-nitrobenzylcarbamate group to induce hypoxia-activated inhibition of O -alkylguanine-DNA alkyltransferase. NBGNU was tested for hypoxic selectivity, cytotoxicity and DNA ICLs ability. Read More

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http://dx.doi.org/10.4155/fmc-2018-0511DOI Listing
December 2018
1 Read

Overcoming the emerging drug resistance of smoothened: an overview of small-molecule SMO antagonists with antiresistance activity.

Future Med Chem 2018 Dec 17;10(24):2855-2875. Epub 2018 Dec 17.

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Ji'nan 250012, PR China.

Hedgehog (HH) signaling pathway plays vital roles in controlling embryonic cell fate and homeostatic, and becomes dormant in mature individuals, aberrant activation of HH signaling pathway is involved in a number of human cancers. Smoothened (SMO), a vital transducer of HH signaling pathway, attracts significant attentions in HH signaling pathway-related cancer therapy. The approval of SMO antagonists vismodegib proves that SMO is a promising therapeutic target, and a number of SMO antagonists are reported since then. Read More

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http://dx.doi.org/10.4155/fmc-2018-0200DOI Listing
December 2018
2 Reads

Discovery of CDK4 inhibitors by convolutional neural networks.

Future Med Chem 2018 Dec 17. Epub 2018 Dec 17.

Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, PR China.

Aim: Descriptors of molecules are important in the discovery of lead compounds. Most of these descriptors are used to represent molecular structures, although structural formulas are the most intuitive representation. Convolutional neural networks (ConvNets) are effective for managing intuitive information. Read More

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http://dx.doi.org/10.4155/fmc-2018-0478DOI Listing
December 2018
2 Reads

Sialic acid as a target for the development of novel antiangiogenic strategies.

Future Med Chem 2018 Dec 12;10(24):2835-2854. Epub 2018 Dec 12.

Section of Experimental Oncology & Immunology, Department of Molecular & Translational Medicine (DMTM), University of Brescia, Brescia 25123, Italy.

Sialic acid is associated with glycoproteins and gangliosides of eukaryotic cells. It regulates various molecular interactions, being implicated in inflammation and cancer, where its expression is regulated by sialyltransferases and sialidases. Angiogenesis, the formation of new capillaries, takes place during inflammation and cancer, and represents the outcome of several interactions occurring at the endothelial surface among angiogenic growth factors, inhibitors, receptors, gangliosides and cell-adhesion molecules. Read More

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https://www.future-science.com/doi/10.4155/fmc-2018-0298
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http://dx.doi.org/10.4155/fmc-2018-0298DOI Listing
December 2018
3 Reads

Design and synthesis of some β-carboline derivatives as multi-target anticancer agents.

Future Med Chem 2018 Dec 12;10(24):2791-2814. Epub 2018 Dec 12.

Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt.

Aim: Some anticancer β-carbolines exhibited dual inhibition of topo-I and KSP.

Methodology/results: Novel β-carbolines were synthesized and screened for their anticancer activity according to the NCI protocol. Five dose assays results indicated that compounds 9, 10, 12, 17 and 20 were potent and non selective anticancer agents; the sulfanyltriazole 12 was the most potent. Read More

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http://dx.doi.org/10.4155/fmc-2018-0226DOI Listing
December 2018
2 Reads

Computational chemical biology on the rise.

Future Med Chem 2019 Jan 10;11(1):1-3. Epub 2018 Dec 10.

Department of Life Science Informatics, B-IT, LIMES Program Unit Chemical Biology & Medicinal Chemistry, Rheinische Friedrich-Wilhelms-Universität, Endenicher Allee 19c, D-53115 Bonn, Germany.

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http://dx.doi.org/10.4155/fmc-2018-0282DOI Listing
January 2019
1 Read

Carbon monoxide and its donors - their implications for medicine.

Future Med Chem 2019 Jan 11;11(1):61-73. Epub 2018 Dec 11.

Department of General Biochemistry, Faculty of Biology & Environmental Protection, University of Lodz, Pomorska 141/3, 90-236 Lodz, Poland.

Inhalation of high concentrations of carbon monoxide (CO) is known to lead to serious systemic complications and neuronal disturbances. However, it has been found that not only is CO produced endogenously, but also that low concentrations can bestow beneficial effects which may be of interest in biology and medicine. As translocation of CO through the human organism is difficult, small molecules known as CO-releasing molecules (CORMs) deliver controlled amounts of CO to biological systems, and these are of great interest from a medical point of view. Read More

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http://dx.doi.org/10.4155/fmc-2018-0215DOI Listing
January 2019
1 Read

Consensus anticancer activity profiles derived from the meta-analysis of reference compounds for widely used cell lines.

Future Med Chem 2019 Jan 11;11(1):33-42. Epub 2018 Dec 11.

Molecular Medicine & Therapeutics Laboratory, CPMB, Osmania University, Hyderabad 500007, India.

Aim: To establish a standard reference for bioactivity of widely used anticancer compounds that might be useful for meaningful interpretation of the cell viability data generated for novel synthetic derivatives.

Materials & Methods: Meta-analysis of published IC50 values was carried out for commonly used anticancer compounds and cell viability experiments were performed to validate the role of certain factors in drug activity.

Results & Conclusion: Variability in the published IC50 values was demonstrated. Read More

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http://dx.doi.org/10.4155/fmc-2018-0303DOI Listing
January 2019
2 Reads

How dynamic docking simulations can help to tackle tough drug targets.

Future Med Chem 2018 Dec 10;10(24):2763-2765. Epub 2018 Dec 10.

Department of Pharmacy & Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.

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http://dx.doi.org/10.4155/fmc-2018-0295DOI Listing
December 2018
1 Read

Discovery of arginine-containing tripeptides as a new class of pancreatic lipase inhibitors.

Future Med Chem 2019 Jan 11;11(1):5-19. Epub 2018 Dec 11.

Department of Pharmacy, G. d'Annunzio University of Chieti-Pescara, Chieti, 66100 Italy.

Aim: The inhibition of pancreatic lipase (PL) represents one of the most promising strategies in the search for novel antiobesity drugs. We propose here a pioneering course by exploring tripeptide scaffolds in the way to selective PL inhibitors.

Methodology/results: The peptide series exhibited good PL inhibitory properties in vitro, with all the strongest inhibitors sharing a central arginine, shown in silico to be relevant for the active site-directed activity. Read More

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http://dx.doi.org/10.4155/fmc-2018-0216DOI Listing
January 2019
1 Read

Synthesis, antiproliferative activity and 2D-QSAR study of some 8-alkyl-2,4-bisbenzylidene-3-nortropinones.

Future Med Chem 2018 Dec 10;10(24):2815-2833. Epub 2018 Dec 10.

Institute of Pharmacy and Molecular Biotechnology, INF364, Heidelberg University, D-69120 Heidelberg, Germany.

Aim: Colon cancer is the third leading cause of death worldwide; therefore, there is a need for an effective therapy with lower side effects.

Methods: A series of 8-alkyl-2,4-bisbenzylidene-3-nortropinones 3 & 14-39 was prepared via Claisen-Schmidt condensation of 8-alkyl-3-nortropinones 11-13 with different aromatic aldehydes. The target compounds were screened for their antiproliferative activity. Read More

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http://dx.doi.org/10.4155/fmc-2018-0205DOI Listing
December 2018
1 Read

Glycans in nanomedicine, impact and perspectives.

Future Med Chem 2019 Jan 11;11(1):43-60. Epub 2018 Dec 11.

Department of Biotechnology & Biosciences, University of Milano-Bicocca, Piazza della Scienza 2, 20126 Milan, Italy.

Glycans have been selected by nature for both structural and 'recognition' purposes. Taking inspiration from nature, nanomedicine exploits glycans not only as structural constituents of nanoparticles and nanostructured biomaterials but also as selective interactors of such glyco-nanotools. Surface glycosylation of nanoparticles finds application in targeting specific cells, whereas recent findings give evidence that the glycan content of cell microenvironment is able to induce the cell fate. Read More

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http://dx.doi.org/10.4155/fmc-2018-0368DOI Listing
January 2019
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Green synthesis and biological activity of silver-curcumin nanoconjugates.

Future Med Chem 2018 Nov 11;10(22):2577-2588. Epub 2018 Dec 11.

National Institute of Laser Enhanced Sciences (NILE), Cairo University, Giza 12613, Egypt.

Aim: There is an urgent need to develop alternative antimicrobial agents and, one of which is via the use of nanotechnology. Green synthetic routes are recently being replaced for nanoparticles preparation. Methods results: Silver-curcumin nanoconjugates (Ag-CurNCs) were prepared in an eco-friendly method. Read More

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http://dx.doi.org/10.4155/fmc-2018-0152DOI Listing
November 2018
1 Read

Novel non-nucleotidic STING agonists for cancer immunotherapy.

Future Med Chem 2018 Dec 10;10(24):2767-2769. Epub 2018 Dec 10.

Department of Neurosurgery, Harvey Cushing Neuro-Oncology Laboratories, Brigham & Women's Hospital, Harvard Medical School, Boston, MA 02115, USA.

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https://www.future-science.com/doi/10.4155/fmc-2018-0367
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http://dx.doi.org/10.4155/fmc-2018-0367DOI Listing
December 2018
5 Reads

One-pot synthesis of spiro(indoline-3,4'-pyrazolo[3,4-b]pyridine)-5'-carbonitriles as p53-MDM2 interaction inhibitors.

Future Med Chem 2018 Dec 10;10(24):2771-2789. Epub 2018 Dec 10.

Department of Applied Organic Chemistry Department, National Research Center, Dokki, Cairo 12622, Egypt.

Aim: Inhibition of P53-mdm2 interaction will lead to cancer cell apoptosis. This strategy was achieved by reported spiro-oxindole derivatives.

Materials & Methods: Spiro(indoline-3,4'-pyrazolo[3,4-b]pyridine)-5'-carbonitrile derivatives (4a-i and 9a, b) were synthesized and screened for their in vitro anticancer activity. Read More

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http://dx.doi.org/10.4155/fmc-2018-0288DOI Listing
December 2018
3 Reads
4.000 Impact Factor

The synthesis and biological evaluation of a new bioactive metabolite of mosapride as a potential gastroprokinetic agent.

Future Med Chem 2019 Jan 11;11(1):21-32. Epub 2018 Dec 11.

Key Laboratory of New Drugs Design & Discovery of Liaoning Province, Shenyang Pharmaceutical University, Shenyang, PR China.

Aim: To synthesize the new bioactive metabolites of mosapride (R)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]-propyl-5-chlorine-4-amino-2-ethoxyben-zamide (R-isomer) and (S)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]-propyl-5-chlorine-4-amino-2-ethoxybenzamide (S-isomer) and evaluate their in vitro and in vivo pharmacological and pharmacokinetic profiles.

Results: S-isomer as a gastroprokinetic agent showed significant pharmacological activities in vivo. Furthermore, compared with the EC values for R-isomer and mosapride, S-isomer was proven to generate the same 5-HT receptor agonistic activity with a smaller amount. Read More

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https://www.future-science.com/doi/10.4155/fmc-2018-0243
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http://dx.doi.org/10.4155/fmc-2018-0243DOI Listing
January 2019
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A computational and experimental study to develop E-selectin targeted peptides for molecular imaging applications.

Future Med Chem 2018 Dec 6. Epub 2018 Dec 6.

Aix Marseille Univ, CNRS, Cent Marseille, ISM2, Marseille, France.

Aim: E-selectin is overexpressed on angiogenic and inflamed endothelium. Molecules binding to E-selectin with high affinity and specificity enable its use as a molecular imaging biomarker.

Material & Methods: The interactions of four different peptides (i. Read More

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http://dx.doi.org/10.4155/fmc-2018-0244DOI Listing
December 2018
14 Reads

Matriptase-2: monitoring and inhibiting its proteolytic activity.

Future Med Chem 2018 Dec 6. Epub 2018 Dec 6.

Department of Molecular Biochemistry, Faculty of Chemistry, University of Gdansk, ul. Wita Stwosza 63, 80-308 Gdansk, Poland.

Matriptase-2 (MT2) is a membrane-anchored proteolytic enzyme. It acts as the proteolytic key regulator in human iron homeostasis. A high expression level can lead to iron overload diseases, whereas mutations in the gene encoding MT2, TMPRSS6, may result in various forms of iron deficiency anemia. Read More

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https://www.future-science.com/doi/10.4155/fmc-2018-0346
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http://dx.doi.org/10.4155/fmc-2018-0346DOI Listing
December 2018
16 Reads

Smart fluorescent probes for in situ imaging of enzyme activity: design strategies and applications.

Future Med Chem 2018 Dec 6. Epub 2018 Dec 6.

School of Chemical Engineering & Pharmacy, Wuhan Institute of Technology, 693 Xiongchu Avenue, Wuhan 430073, PR China.

Enzymes play critical roles in the physiological and pathological processes of living systems. To provide detailed pictures of enzyme activity at the molecular and cellular levels, interdisciplinary studies of chemistry and biology have led to the emergence of many smart fluorescent probes, which emit fluorescence or show a shifted signal only upon interaction with their targets. With distinct advantage of a higher signal-to-noise ratio than traditional 'always on' probes, smart fluorescent probes enable sensitive detection of enzymes with clinical significance. Read More

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http://dx.doi.org/10.4155/fmc-2018-0193DOI Listing
December 2018
1 Read

Anti-inflammatory indomethacin analogs endowed with preferential COX-2 inhibitory activity.

Future Med Chem 2018 Dec 6. Epub 2018 Dec 6.

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt.

Aim: The undeniable indomethacin potency has always suffered serious obstacles such as gastric damage. Continuous attempts to develop potent yet safe indomethacin analogs have never ceased.

Results: Herein are new indole derivatives 4a-h and 5a-c, which were synthesized via Fisher indole reaction, evaluated for both their in vivo anti-inflammatory activities using rat paw edema method and their in vitro cyclooxygenase inhibitory activities. Read More

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http://dx.doi.org/10.4155/fmc-2018-0224DOI Listing
December 2018
3 Reads