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5.187 Aktuelle Fachpublikationen in Journal of Medicinal Chemistry

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Design, Synthesis, and in Vitro and in Vivo Evaluation of Ouabain Analogues as Potent and Selective Na,K-ATPase α4 Isoform Inhibitors for Male Contraception

19.01.2018 | Shameem Sultana Syeda; Gladis Sánchez; Kwon Ho Hong; Jon E. Hawkinson; Gunda I. Georg; Gustavo Blanco, Journal of Medicinal Chemistry, 2018

Na,K-ATPase α4 is a testis-specific plasma membrane Na+ and K+ transporter expressed in sperm flagellum. Deletion of Na,K-ATPase α4 in male mice results in complete infertility, making it an attractive target for male contraception. Na,K-ATPase α4 is characterized by a high affinity for the ...

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Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors

19.01.2018 | Bin Yang; Melissa M. Vasbinder; Alexander W. Hird; Qibin Su; Haixia Wang; Yan Yu; Dorin Toader; Paul D. Lyne; Jon A. ..., Journal of Medicinal Chemistry, 2018

Checkpoint kinase 1 (CHK1) inhibitors are potential cancer therapeutics that can be utilized for enhancing the efficacy of DNA damaging agents. Multiple small molecule CHK1 inhibitors from different chemical scaffolds have been developed and evaluated in clinical trials in combination with ...

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Structural Modification of Natural Product Tanshinone I Leading to Discovery of Novel Nitrogen-Enriched Derivatives with Enhanced Anticancer Profile and Improved Drug-like Properties

19.01.2018 | Chunyong Ding; Qianting Tian; Jie Li; Mingkun Jiao; Shanshan Song; Yingqing Wang; Zehong Miao; Ao Zhang, Journal of Medicinal Chemistry, 2018

The clinical development of natural product tanshinone I (1) for cancer therapy is hampered by its weak potency and poor drug-like properties. Herein, a more broad and systemic structural modification on 1 was conducted to generate four series of new tanshinone derivatives. Among them, the lactam ...

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Oligoethyleneoxy-Modified 99mTc-Labeled β-Amyloid Imaging Probes with Improved Brain Pharmacokinetics for Single-Photon Emission Computed Tomography

18.01.2018 | Xiaoyang Zhang; Yaqin Hou; Cheng Peng; Chu Wang; Xiang Wang; Zhigang Liang; Jing Lu; Baian Chen; Jiapei Dai; Boli Li ..., Journal of Medicinal Chemistry, 2018

An oligoethyleneoxy linker was introduced for conjugation between 99mTc/Re-bis(aminoethanethiol) (BAT) and β-amyloid (Aβ) binding scaffolds. Rhenium complexes exhibited high to moderate binding affinity to Aβ1–42 aggregates and efficient fluorescent staining to Aβ plaques in brain tissue. After ...

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Lipidated Brartemicin Analogues Are Potent Th1-Stimulating Vaccine Adjuvants

18.01.2018 | Amy J. Foster; Masahiro Nagata; Xiuyuan Lu; Amy T. Lynch; Zakaria Omahdi; Eri Ishikawa; Sho Yamasaki; Mattie S. M. T ..., Journal of Medicinal Chemistry, 2018

Effective Th1-stimulating vaccine adjuvants typically activate antigen presenting cells (APCs) through pattern recognition receptors (PRRs). Macrophage inducible C-type lectin (Mincle) is a PRR expressed on APCs and has been identified as a target for Th1-stimulating adjuvants. Herein, we report ...

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In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses

17.01.2018 | Yuanxiang Wang; Yanmei Hu; Shuting Xu; Yongtao Zhang; Rami Musharrafieh; Raymond Kin Hau; Chunlong Ma; Jun Wang, Journal of Medicinal Chemistry, 2018

Influenza viruses are respiratory pathogens that are responsible for both seasonal influenza epidemics and occasional influenza pandemics. The narrow therapeutic window of oseltamivir, coupled with the emergence of drug resistance, calls for the next-generation of antivirals. With our continuous ...

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Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors

17.01.2018 | Mohammed I. El-Gamal; Shahad K. Al-Ameen; Dania M. Al-Koumi; Mawadda G. Hamad; Nouran A. Jalal; Chang-Hyun Oh, Journal of Medicinal Chemistry, 2018

Colony stimulation factor-1 receptor (CSF-1R), which is also known as FMS kinase, plays an important role in initiating inflammatory, cancer, and bone disorders when it is overstimulated by its ligand, CSF-1. Innate immunity, as well as macrophage differentiation and survival, are regulated by ...

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MetaQSAR: An Integrated Database Engine to Manage and Analyze Metabolic Data

17.01.2018 | Alessandro Pedretti; Angelica Mazzolari; Giulio Vistoli; Bernard Testa, Journal of Medicinal Chemistry, 2018

The study describes the MetaQSAR tool, a new database engine specifically tailored to collect and analyze metabolic data. This is a plug-in embedded in the VEGA suite of programs (freely downloadable at www.vegazz.net) and takes advantage from all cheminformatics features implemented in the ...

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Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate

16.01.2018 | Christopher J. Helal; Eric Arnold; Tracey Boyden; Cheng Chang; Thomas A. Chappie; Ethan Fisher; Mihaly Hajos; John F ..., Journal of Medicinal Chemistry, 2018

Computational modeling was used to direct the synthesis of analogs of previously reported phosphodiesterase 2A (PDE2A) inhibitor 1 with an imidazotriazine core to yield compounds of significantly enhanced potency. The analog PF-05180999 (30) was subsequently identified as a preclinical candidate ...

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Target Identification and Mode of Action of Four Chemically Divergent Drugs against Ebolavirus Infection

16.01.2018 | Jingshan Ren; Yuguang Zhao; Elizabeth E. Fry; David I. Stuart, Journal of Medicinal Chemistry, 2018

Here, we show that four chemically divergent approved drugs reported to inhibit Ebolavirus infection, benztropine, bepridil, paroxetine and sertraline, directly interact with the Ebolavirus glycoprotein. Binding of these drugs destabilizes the protein, suggesting that this may be the mechanism of ...

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