Welcome to EndNote™ ... Our biggest sale yet! Save 25% on EndNote 21 single-user licenses until March 31st, 2024!§Cancer Research UK Drug Discovery Unit, Paterson Institute for Cancer Research, University of Manchester, Wilmslow Road, Manchester, M20 4BX, U.K.2013 Philip S. Portoghese Medicinal Chemistry Lectureship: Drug Discovery Targeting Allosteric Sites †. Craig W. Lindsley *. Journal of Medicinal Chemistry 2014, 57, 18, 7485-7498 (Perspective) Publication Date (Web): September 2, 2014. Abstract.The use of deuteration in medicinal chemistry has exploded in the past years, and the FDA has recently approved the first deuterium-labeled drug. Precision deuteration goes beyond the pure and simple amelioration of the pharmacokinetic parameters of a drug and might provide an opportunity when facing problems in terms of metabolism-mediated toxicity, drug …The figure depicts the surface and cartoon representations of HDAC3 crystal structure (orange) along with the docked conformation of the preclinical candidate ST7612AA1 (green). The zinc ion in the catalytic site is represented as a purple sphere. (Giannini, G.; et al. J. Med. Chem. 2014, 57, 8358–8377) View the article.Medicinal chemistry articles from across Nature Portfolio. Medicinal chemistry deals with the design, optimization and development of chemical compounds for use as drugs. It is inherently a ...The more sound and complete your science is, the more utility it will have for the medicinal chemistry community and the more your work will be cited and your tool compounds studied. Pharmacokinetic–pharmacodynamic relationships are at the center of successful drug discovery. If you have questions, please email an editor with a presubmission inquiry. Journal …Through virtual screening and structural optimization, a potent DYRK2 inhibitor 43 was obtained, which displayed high kinase selectivity, great water solubility, favorable safety properties, and significant anti-prostate cancer activity. Furthermore, the detailed interactions between 43 and DYRK2 were illustrated by the cocrystals. View the article.Medicinal Chemistry. Impact Factor: 2.3. Indexed in: Scopus, SCI Expanded, MEDLINE/PubMed... View all. Volume 20 , Issues 10, 2024. Back Journal Home. …In 2022, 23 new small molecule chemical entities were approved as drugs by the United States FDA, European Union EMA, Japan PMDA, and …Medicinal chemistry has evolved rapidly into a highly interdisciplinary field, enriched by the collaborative efforts of experts from a wide spectrum of …ProTide and cyclic phosphate ester are two successful prodrug technologies to overcome the limitations of nucleoside drugs, among which the cyclic phosphate ester strategy has not been widely used in the optimization of gemcitabine. Herein, we designed a series of novel ProTide and cyclic phosphate ester prodrugs of gemcitabine. Cyclic …Read current and featured research from the Journal of Medicinal Chemistry on ACS Publications, a trusted source for peer-reviewed journals.In chemistry, the atom is the most fundamental building block of matter. Now the automotive world has its atom -- a car so pure and simple that some people are calling it minimalis... Akane Kawamura *. Journal of Medicinal Chemistry, Articles ASAP (Article) Publication Date (Web): January 31, 2024. Abstract. Full text. PDF. ABSTRACT. Read the latest ASAP articles from the Journal of Medicinal Chemistry on ACS Publications, a trusted source for peer-reviewed journals. Medicinal Chemistry Research is a journal focused on the publication of novel findings in drug design, drug discovery, and mechanisms of action of biologically …Read the latest articles of Medicinal Chemistry at ScienceDirect.com, Elsevier’s leading platform of peer-reviewed scholarly literature.Feb 8, 2024 · Issue Publication Information. Journal of Medicinal Chemistry2024, 67, 3, XXX-XXX (Article) Publication Date (Web):February 8, 2024. First Page. PDF. Read research published in the Journal of Medicinal Chemistry Vol. 67 Issue 3 on ACS Publications, a trusted source for peer-reviewed journals. Dec 31, 2020 · Spirocyclic scaffolds are incorporated in various approved drugs and drug candidates. The increasing interest in less planar bioactive compounds has given rise to the development of synthetic methodologies for the preparation of spirocyclic scaffolds. In this Perspective, we summarize the diverse synthetic routes to obtain spirocyclic systems. The impact of spirocycles on potency and ... Nov 22, 2023 · The identification of clinical candidate LY3522348 (compound 23) is described. LY3522348 is a highly selective, oral dual inhibitor of human ketohexokinase isoforms C and A (hKHK-C, hKHK-A). Optimization began with highly efficient (S)-2-(2-methylazetidin-1-yl)-6-(1H-pyrazol-4-yl)-4-(trifluoromethyl)nicotinonitrile (3). Efforts focused on developing absorption, distribution, metabolism ... Most of us have learned the hard way that there’s a certain technique to pouring our beer without making it overflow and ruin everything. You have to strategically tilt the glass a...The Journal of Medicinal Chemistry is a peer-reviewed medical journal covering research in medicinal chemistry. It is published by the American Chemical Society. It was established in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry and obtained its current name in 1963.About the journal. Aims & Scope. EJMECH (The European Journal of Medicinal Chemistry) is a global journal that publishes studies on the main aspects of …Cubane is a highly strained saturated hydrocarbon system that has historically been of interest in theoretical organic chemistry. More recently it has become a molecule of interest for biological applications due to its inherent stability and limited toxicity. Of greater significance is the ability to potentially functionalize cubane at each of its …Sep 21, 2023 · Medicinal Chemistry. Trust ACS to bring you experimental and theoretical studies across a broad range of medicinal chemistry, including compound design and optimization, biological evaluation, molecular mechanistic understanding of drug delivery and drug delivery systems, imaging agents, and pharmacology and translational science of both small and large bioactive molecules. Dey 23, 1401 AP ... ... Medicinal Chemistry Publications in 2021”; J M... Walsh et al., “Fragment-to-Lead Medicinal Chemistry Publications in 2021”; J Med Chem 2023.ACS Publications is pleased to announce that Craig W. Lindsley, Ph.D., has been named as Editor-in-Chief (EIC) of the Journal of Medicinal Chemistry. His term is set to begin on January 1, 2021. Lindsley is the William K. Warren, Jr., chair in medicine at Vanderbilt University. There, he is a University Professor of Pharmacology, …Research and review articles in medicinal chemistry and related drug discovery science. Editor-in-chief: Mike Waring Impact Factor: 4.1 Time to first decision (peer reviewed only): 30 days. Submit your article Opens in new window Information and templates for authors Search this journal. Find an article. Year. Page . Find issues by year (2020 - Present) Related journals. …Journal of Medicinal Chemistry Vol. 61 No. 9 - ACS Publications. May 10, 2018 Volume 61, Issue 9 Pages 3755-4272. About the Cover: Conformational flexibility …Feb 11, 2021 · The cover shows Janus kinase 1, a tyrosine kinase involved in cytokine signaling that is a therapeutic target for inflammatory disorders and autoimmune diseases. In their Perspective, Xie et al. highlight nononcologic applications of kinase inhibitors. Image credit: Shutterstock. View the article. KRASG12D, the most frequent KRAS oncogenic mutation, is a promising target for cancer therapy. Herein, we report the design, synthesis, and biological evaluation of a series of KRASG12D PROTACs by connecting the analogues of MRTX1133 and the VHL ligand. Structural modifications of the linker moiety and KRAS inhibitor part suggested a critical role of …Medicinal Chemistry. Recent Highlights in our Medicinal Chemistry Research: ... J. 2017, 23, 3126–3138.call_made · external pageQ.A. Huchet, N. Trapp, B. Kuhn ...Khordad 5, 1396 AP ... PDF | The editorial letter for the new journal on medicinal chemistry and drug discovery.... | Find, read and cite all the research you need ...Tumor necrosis factor receptor-associated protein 1 (TRAP1) is a mitochondrial molecular chaperone modulating cellular metabolism and signaling pathways by altering the conformation, activity, and stability of numerous substrate proteins called clients. It exerts its chaperone function as an adaptive response to counter cellular …Medicinal Chemistry Research is a journal focused on the publication of novel findings in drug design, drug discovery, and mechanisms of action of biologically …Oct 12, 2012 · The incorporation of silicon and synthesis of organosilicon small molecules provide unique opportunities for medicinal applications. The biological investigation of organosilicon small molecules is particularly interesting because of differences in their chemical properties that can contribute to enhanced potency and improved pharmacological attributes. Applications such as inhibitor design ... Journal of Medicinal Chemistry2022, 65, 12, 8113-8126 (Perspective) Publication Date (Web):June 3, 2022. Abstract. Full text. PDF. ABSTRACT. Targeted protein degradation has become a reliable tool in the medicinal chemist’s toolbox, as seen with rapid progression of PROTACs (proteolysis targeting chimeras) to clinic. Nov 23, 2023 · Issue Publication Information. Journal of Medicinal Chemistry 2023, 66, 22, XXX-XXX (Article) Publication Date (Web): November 23, 2023. First Page. PDF. Read research published in the Journal of Medicinal Chemistry Vol. 66 Issue 22 on ACS Publications, a trusted source for peer-reviewed journals. Azar 24, 1399 AP ... “The Journal of Medicinal Chemistry plays a critical role in not only disseminating the most important advances in drug discovery, but also in ...Addressing resistance to third-generation EGFR TKIs such as osimertinib via the EGFRC797S mutation remains a highly unmet need in EGFR-driven non-small-cell lung cancer (NSCLC). Herein, we present the discovery of the allosteric EGFR inhibitor 57, a novel fourth-generation inhibitor to overcome EGFRC797S-mediated resistance in …For oral drugs, medicinal chemists aim to design compounds with high oral bioavailability, of which permeability is a key determinant. Taking advantage of >2000 compounds tested in rat bioavailability studies and >20,000 compounds tested in Caco2 assays at Bayer, we have examined the molecular properties governing bioavailability …Current estimates of the cost to bring a single drug to market are in excess of 2–3 billion dollars. A significant portion of this cost may be attributed to two factors: the historically high attrition of candidate Advances in both computer hardware and in silico methods aim to expedite as well as improve various aspects of the medicinal chemistry’s quintessential design-make-test …Journal of Medicinal Chemistry (2014), 57 (8), 3186-3204 CODEN: JMCMAR; ISSN: 0022-2623. (American Chemical Society) A review. Similarity is a subjective and multifaceted concept, regardless of whether compds. or any other objects are considered. Despite its intrinsically subjective nature, attempts to quantify the similarity of compds. …Journal of Medicinal Chemistry2022, 65, 12, 8113-8126 (Perspective) Publication Date (Web):June 3, 2022. Abstract. Full text. PDF. ABSTRACT. Targeted protein degradation has become a reliable tool in the medicinal chemist’s toolbox, as seen with rapid progression of PROTACs (proteolysis targeting chimeras) to clinic.Medicinal chemistry is a rapidly maturing discipline. Understanding the relationship between structure and function is crucial to understand the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight and facilitate the discovery and development of new therapeutic agents to …In chemistry, the atom is the most fundamental building block of matter. Now the automotive world has its atom -- a car so pure and simple that some people are calling it minimalis...The use of an acetylene (ethynyl) group in medicinal chemistry coincides with the launch of the Journal of Medicinal Chemistry in 1959. Since then, the acetylene group has been broadly exploited in drug discovery and development. As a result, it has become recognized as a privileged structural feature for targeting a wide range of … » JOURNAL OF MEDICINAL CHEMISTRY. Abbreviation: J MED CHEM ISSN: 0022-2623 eISSN: 1520-4804 Category / Quartile: CHEMISTRY, MEDICINAL - SCIE(Q1) Journal of Medicinal Chemistry 2019, 62, 9, XXX-XXX (Article) Publication Date (Web): May 9, 2019. PDF. Read research published in the Journal of Medicinal Chemistry Vol. 62 Issue 9 on ACS Publications, a trusted source for peer-reviewed journals.Read the latest articles of Current Medicinal Chemistry at ScienceDirect.com, Elsevier’s leading platform of peer-reviewed scholarly literature.Read current and featured research from the Journal of Medicinal Chemistry on ACS Publications, a trusted source for peer-reviewed journals.The discovery and development of small-molecule therapeutics effective against Gram-negative pathogens are highly challenging tasks. Most compounds that are active in biochemical settings fail to exhibit whole-cell activity. The major reason for this lack of activity is the effectiveness of bacterial cell envelopes as permeability barriers. These …Article processing charges (APCs) apply to articles that are accepted for publication by our external editors, following rigorous peer review. See all (966) Specialty Chief Editor. Putra Malaysia University. Selangor Darul Ehsan, Malaysia. Associate Editor. Medicinal and Pharmaceutical Chemistry.David W. Dunwell. and. Delme Evans. Journal of Medicinal Chemistry 1977, 20, 6, 797-801 (Article) Publication Date (Print): June 1, 1977. First Page. PDF. 3,4-Methylenedioxyphenyl-, isopropylidenedioxyphenyl-, and benzyl-substituted chiral 2-aminosuccinimides and 3-aminopyrrolidines. Stereoselective investigations of potential …Khordad 16, 1402 AP ... However, our oxazole-based compounds turned out to be effective in cellular models of neurodegenerative diseases mechanisms, and had disease- ...ACS Medicinal Chemistry Letters is a Transformative Journal. ACS Medicinal Chemistry Letters has been certified as a transformative journal by cOAlition S, committing to a transition to 100% open access in the future. If your research funder has signed Plan S, your open access charges may be covered by your funder through December 31, 2024.Microtubules play a crucial role in multiple cellular functions including mitosis, cell signaling, and organelle trafficking, which makes the microtubule an important target for cancer therapy. Despite the great successes of microtubule-targeting agents in the clinic, the development of drug resistance and dose-limiting toxicity restrict their clinical …ACS Medicinal Chemistry Letters is a Transformative Journal. ACS Medicinal Chemistry Letters has been certified as a transformative journal by cOAlition S, committing to a transition to 100% open access in the future. If your research funder has signed Plan S, your open access charges may be covered by your funder through December 31, 2024.This journal publishes research on chemical compounds for therapeutic use. It covers natural and syhthetic medicines. newsletter banner. Search anything here. Login. Login. Remember Me. ... Medicinal Chemistry . Impact Factor: 2.3. Indexed in: Scopus, SCI Expanded, MEDLINE/PubMed... View all. Volume 20 , Issues 10, 2024. Back Journal Home. Call For …Jul 24, 2017 · Over the past decade, peptide drug discovery has experienced a revival of interest and scientific momentum, as the pharmaceutical industry has come to appreciate the role that peptide therapeutics can play in addressing unmet medical needs and how this class of compounds can be an excellent complement or even preferable alternative to small molecule and biological therapeutics. In this ... Medicinal chemistry is a fast-evolving interdisciplinary research area which aims to improve human life by developing drugs to combat diseases. Nature Communications interviewed three scientists ...Medicinal chemistry and dynamic structure-activity analysis in the discovery of drugs acting at histamine H2 receptors. Robin Ganellin. Journal of Medicinal Chemistry 1981, 24, 8, 913-920 (Article) Publication Date (Print): August 1, 1981. First Page.Read the latest articles of Anti-Cancer Agents in Medicinal Chemistry at ScienceDirect.com, Elsevier’s leading platform of peer-reviewed scholarly …Eur J Med Chem 211, 113109. CNIO Publication. Martínez-González S, Alvarez RM, Martín JI, García AB, Riesco-Fagundo C, Varela C, Rodríguez Hergueta ...Azar 24, 1399 AP ... “The Journal of Medicinal Chemistry plays a critical role in not only disseminating the most important advances in drug discovery, but also in ...Enhanced activity against multidrug resistant bacteria through coapplication of TPAD, an analogue of tachyplesin I (β-strand in light blue) and LED209, that is an inhibitor of the QseC/B signaling pathway (ball in orange or green). The horseshoe crabs are shown in cyan, and bacteria are shown in gray. (Yu, R.; et al. J. Med. Chem. 2020, 63, DOI: …. Medicinal chemistry articles from across Nature Portfolio. Medicinal Medicinal chemistry, in its crudest sense, has been practi Spirocyclic Scaffolds in Medicinal Chemistry J Med Chem. 2021 Jan 14;64(1):150-183. doi: 10.1021/acs.jmedchem.0c01473. Epub 2020 Dec 31. Authors Kerstin Hiesinger 1 , Dmitry Dar'in 2 , Ewgenij Proschak 1 , Mikhail Krasavin 2 Affiliations 1 Institute of Pharmaceutical Chemistry, Goethe University, Max-von-Laue Straße 9, D ... Medicinal chemistry has evolved rapidly into a highl The stimulation of soluble guanylate cyclase is an attractive approach to treat patients with resistant hypertension. The discovery of BAY-747, an oral sGC stimulator with excellent DMPK and preclinical pharmacology profile from a screening hit, is described. The asset is in clinical development and shows long-lasting pharmacological effects. View the … eISBN: 9781734427455. DOI: 10.1021/mc-2022-vol57. Joanne J....
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