J medicinal chemistry

Rapid emergence of tumor resistance via RAS pathway reactivation has been reported from clinical studies of covalent KRASG12C inhibitors. Thus, inhibitors with broad potential for combination treatment and distinct binding modes to overcome resistance mutations may prove beneficial. JDQ443 is an investigational covalent KRASG12C …

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 ... The Journal of Medicinal Chemistry is a leading journal in the field, and we openly encourage submissions from drug discovery scientists globally—we are committed to evaluate each submission with the same editorial standards regardless of geographical, age, gender, or sector identity of the authors. We want your best research! We look forward to working with all of you …Each year, new drugs are introduced to the market, representing structures that have affinity for biological targets implicated in human diseases and conditions. These new chemical entities (NCEs), particularly small molecules and antibody–drug conjugates, provide insight into molecular recognition and serve as potential leads for the design of future …Aims and Scope · Drug delivery · Drug design and discovery · Drug metabolism · Drug target · Diseases: Research and Treatment · Natural pr...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. …Retraction of “CNS Physicochemical Property Space Shaped by a Diverse Set of Molecules with Experimentally Determined Exposure in the Mouse Brain”. Zoran Rankovic. Journal of Medicinal Chemistry 2019, 62, 3, 1699 (Retraction) Publication Date (Web): February 5, 2019. Full text.

About the journal. Aims & Scope. EJMECH (The European Journal of Medicinal Chemistry) is a global journal that publishes studies on the main aspects of …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. Chemistry is basic to essentially every field of science. A working knowledge of chemistry informs medicine, energy production and the vast majority of industrial processes.In the field of chemistry, staying up-to-date with the latest research is crucial for scientific advancement. One prominent publisher that has significantly contributed to the diss...In the field of chemistry, staying up-to-date with the latest research is crucial for scientific advancement. One prominent publisher that has significantly contributed to the diss...

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 ...The Journal of Medicinal Chemistry, ACS Medicinal Chemistry Letters, ACS Bio & Med Chem Au, Journal of Natural Products, ACS Chemical Neuroscience, and ACS Chemical Biology are welcoming submissions to a Virtual Special Issue showcasing the latest research on natural products driven medicinal chemistry. The submission deadline is April 30, 2024. Read the …Journal of Medicinal Chemistry (2018), 61 (9), 4189-4202 CODEN: JMCMAR; ISSN: 0022-2623. (American Chemical Society) Conformational flexibility has been proposed to significantly affect drug properties outside rule-of-5 (Ro5) chem. space. Here, we investigated the influence of dynamically exposed polarity on cell permeability and aq. …Retraction of “CNS Physicochemical Property Space Shaped by a Diverse Set of Molecules with Experimentally Determined Exposure in the Mouse Brain”. Zoran Rankovic. Journal of Medicinal Chemistry 2019, 62, 3, 1699 (Retraction) Publication Date (Web): February 5, 2019. Full text.

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Cyclin-dependent kinase 8 (CDK8), as a kinase subunit of the Mediator complex, is involved in the regulation of RNA polymerase II-mediated transcription, thereby modulating multiple signaling pathways and multiple transcription factors involved in oncogenic control. CDK8 deregulation has been implicated in human diseases, …2010 — Volume 45. 2009 — Volume 44. 2008 — Volume 43. 2007 — Volume 42. 2006 — Volume 41. 2005 — Volume 40. Page 1 of 2. ISSN: 0223-5234. Read the latest articles of European Journal of Medicinal Chemistry at ScienceDirect.com, Elsevier’s leading platform of peer-reviewed scholarly literature. 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: 10.1021/acs.jmedchem.9b01563) View the article. Cyclin-dependent kinase 8 (CDK8), as a kinase subunit of the Mediator complex, is involved in the regulation of RNA polymerase II-mediated transcription, thereby modulating multiple signaling pathways and multiple transcription factors involved in oncogenic control. CDK8 deregulation has been implicated in human diseases, …Eur J Med Chem 211, 113109. CNIO Publication. Martínez-González S, Alvarez RM, Martín JI, García AB, Riesco-Fagundo C, Varela C, Rodríguez Hergueta ...Bahman 10, 1391 AP ... S. E. Morozova, K. A. Esikov, V. Yu. Zubarev, A. A. Malin, V. A. Ostrovskii, Zh. Org. Khim., 2004, 40, 1576 [Russ. J. Org. Chem. (Engl. Transl.) ...

Medicinal chemistry or pharmaceutical chemistry is the chemistry discipline concerned with the design, development and synthesis of pharmaceutical drug s. The discipline combines expertise from chemistry and pharmacology to identify, develop and synthesize chemical agents that have a therapeutic use and to evaluate the properties of …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 …The Journal of Medicinal Chemistry publishes studies that contribute to an understanding of the relationship between molecular structure and biological activity or mode of action. Some specific areas that are appropriate include the following: -Design, synthesis, and biological evaluation of novel biologically active compounds, diagnostic ...Medicinal chemistry, Peptides and proteins, Pharmaceuticals, The first issue ever published by the Journal of Medicinal Chemistry dates to 1959 (at that time it was the Journal of Medicinal and Pharmaceutical Chemistry ). Looking at some of the articles included, it was reported, for example, how the combination of hydralazine and reserpine ...Pharmaceutical and medicinal significance of sulfur (S VI)-Containing motifs for drug discovery: A critical review Chuang Zhao, K.P. Rakesh, L. Ravidar, Wan-Yin Fang, Hua-Li Qin Pages 679-734Brian R. De Costa. , Richard B. Rothman. , Victor Bykov. , Arthur E. Jacobson. , and. Kenner C. Rice. Journal of Medicinal Chemistry 1989, 32, 2, 281-283 (Article) …EJMCR (European Journal of Medicinal Chemistry Reports) is an open access companion title to European Journal of Medicinal Chemistry. It is an international open access journal indexed in Scopus and the Impact Factor will be announced soon. EJMCR publishes all aspects of medicinal chemistry with a focus on drug discovery. It provides …Ordibehesht 7, 1401 AP ... ISSN 0022-2623 (Print) | Journal of medicinal chemistry.Journal of Medicinal Chemistry (2018), 61 (9), 4189-4202 CODEN: JMCMAR; ISSN: 0022-2623. (American Chemical Society) Conformational flexibility has been proposed to significantly affect drug properties outside rule-of-5 (Ro5) chem. space. Here, we investigated the influence of dynamically exposed polarity on cell permeability and aq. …Medicinal chemistry, a unique component of the pharmacy curriculum, imparts vital knowledge and critical-thinking skills to pharmacy students and sets them apart as chemical experts among health care professionals. 33 This specialized set of proficiencies in medicinal chemistry and drug discovery, poises the pharmacist as the …

publication in Journal of Medicinal Chemistry, the “production step” was identified (as best as possible), which was the step ultimately yielding final screening compounds. For natural product total synthesis papers, 30 papers were selected from 2014 to 2015 publications from both the Journal of the American

The emergence of resistance to PARP1 inhibitors poses a current therapeutic challenge, necessitating the development of novel strategies to overcome this …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, …Medicinal chemistry or pharmaceutical chemistry is the chemistry discipline concerned with the design, development and synthesis of pharmaceutical drug s. The discipline combines expertise from chemistry and pharmacology to identify, develop and synthesize chemical agents that have a therapeutic use and to evaluate the properties of …Journal of Medicinal Chemistry (2020), 63 (23), 14805-14820 CODEN: JMCMAR; ISSN: 0022-2623. (American Chemical Society) UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC) is a zinc metalloenzyme that catalyzes the first committed step in the biosynthesis of Lipid A, an essential component of the cell …PDF | On Aug 12, 2015, Kishna Ram Senwar and others published European Journal of Medicinal Chemistry | Find, read and cite all the research you need on ...The urea functionality is inherent to numerous bioactive compounds, including a variety of clinically approved therapies. Urea containing compounds are increasingly used in medicinal chemistry and drug design in order to establish key drug–target interactions and fine-tune crucial drug-like properties. In this perspective, we highlight …Recently, there has been an increasing use of the cyclopropyl ring in drug development to transition drug candidates from the preclinical to clinical stage. Important features of the cyclopropane ring are, the (1) coplanarity of the three carbon atoms, (2) relatively shorter (1.51 Å) C–C bonds, (3) enhanced π-character of C–C bonds, and (4) C–H bonds are shorter …

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Building on recent advances in peptide science, medicinal chemists have developed a hybrid class of bioconjugates, called peptide–drug conjugates, that demonstrate improved efficacy compared to peptides and small molecules independently. In this Perspective, we discuss how the conjugation of synergistic peptides and small molecules can be used to overcome complex …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 …Corrigendum to “Design and synthesis of highly TRAIL expression HDAC inhibitors based on ONC201 to promote apoptosis of colorectal cancer” [Eur. J. Med. Chem. 238 (2022) 1–20/114484] Hao Cui, Zan Hu, Kang Yang, Jingkun Huang, ...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. The H1047R mutation of PIK3CA is highly prevalent in breast cancers and other solid tumors. Selectively targeting PI3KαH1047R over …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.Medicinal chemistry has evolved rapidly into a highly interdisciplinary field, enriched by the collaborative efforts of experts from a wide spectrum of specialist areas, from chemoinformaticians and physical chemists to molecular biologists and pharmacologists. Future Medicinal Chemistry provides a regular point of access to commentary and debate for this …Apr 27, 2023 · Journal of Medicinal Chemistry 2023, 66, 8, XXX-XXX (Article) Publication Date (Web): April 27, 2023. PDF. Read research published in the Journal of Medicinal Chemistry Vol. 66 Issue 8 on ACS Publications, a trusted source for peer-reviewed journals. Journal of Medicinal Chemistry. Findings on the relationship between molecular structure and biological activity or mode of action in drug discovery and … ….

Journal of Medicinal Chemistry2022, 65, 10, 7106-7117 (Article) Publication Date (Web):May 17, 2022. Abstract. Full text. PDF. ABSTRACT. Hypoxia is a feature of most solid tumors and a key determinant of cancer growth and propagation. Sensing hypoxia effectively could lead to more favorable clinical outcomes. 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. Issue Publication Information. Journal of Medicinal Chemistry 2024, 67, 2, XXX-XXX (Article) Publication Date (Web): January 25, 2024. First Page. PDF. Read research published in the Journal of Medicinal Chemistry Vol. 67 Issue 2 on ACS Publications, a trusted source for peer-reviewed journals.Stabilization of hypoxia-inducible factor (HIF) by inhibiting prolyl hydroxylase domain enzymes (PHDs) represents a breakthrough in treating anemia associated with chronic kidney disease. Here, we identified a novel scaffold for noncarboxylic PHD inhibitors by utilizing structure-based drug design (SBDD) and generative models. Iterative …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 …A first and highly selective radiolabeled TrkB/C receptor kinase inhibitor permeates the blood­– brain barrier in multiple species, including a human subject, and offers new possibilities for PET imaging of the living brain. (Bernard-Gauthier, V.; et al. J. Med. Chem. 2017, 60, DOI: 10.1021/acs.jmedchem.7b00396) View the article.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 …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. The Journal of Medicinal Chemistry is a leading journal in the field, and we openly encourage submissions from drug discovery scientists globally—we are committed to evaluate each submission with the same editorial standards regardless of geographical, age, gender, or sector identity of the authors. We want your best research! Sep 25, 2014 · Nitrogen heterocycles are among the most significant structural components of pharmaceuticals. Analysis of our database of U.S. FDA approved drugs reveals that 59% of unique small-molecule drugs contain a nitrogen heterocycle. In this review we report on the top 25 most commonly utilized nitrogen heterocycles found in pharmaceuticals. The main part of our analysis is divided into seven ... J medicinal chemistry, In our cover art, we incorporated elements from Chinese classical culture and symbolized the equipment for drug preparation with an alchemy furnace. The compound (S)-XY-05, which we have developed, effectively enters tumor cells and specifically inhibits PARP7. As a result, T cells are recruited and activated, leading to the destruction of tumor cells. To depict …, GABA-Activated Ligand Gated Ion Channels: Medicinal Chemistry and Molecular Biology. Mary Chebib. and. Graham A. R. Johnston. Journal of Medicinal Chemistry 2000, 43, 8, 1427-1447 (Perspective) Publication Date (Web): March 30, 2000. First Page., Journal of Medicinal Chemistry 2001, 44, 4, 633-640 (Article) Publication Date (Web): January 12, 2001. Abstract. Full text. PDF. ABSTRACT. Read research published in the Journal of Medicinal Chemistry Vol. 44 Issue 4 on ACS Publications, a trusted source for peer-reviewed journals. , The Medicinal Chemistry Section of the journal Molecules publishes original research and review articles that increase our understanding of how the chemical structure of bioactive molecules determines their pharmacodynamic, pharmacokinetic, and physicochemical properties and, hence, their therapeutic potential. In particular, this …, The journal publishes reports of experimental results in medicinal chemistry, chemical biology and drug discovery and design, emphasizing new and emerging advances and concepts in these fields. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction ... , 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: 10.1021/acs.jmedchem.9b01563) View the article. , Chemical Biology Letters · Journal of Integrated Science and Technology · Journal of Biomedical and Therapeutic Sciences · Journal of Materials Nanoscience&nbs..., Tir 16, 1400 AP ... ... chemistry-related information and research through its multiple databases, peer-reviewed journals and scientific conferences. Join the ..., 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. , Bahman 10, 1391 AP ... S. E. Morozova, K. A. Esikov, V. Yu. Zubarev, A. A. Malin, V. A. Ostrovskii, Zh. Org. Khim., 2004, 40, 1576 [Russ. J. Org. Chem. (Engl. Transl.) ..., 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. , Journal of Medicinal Chemistry 2018, 61, 13, XXX-XXX (Article) Publication Date (Web): July 12, 2018. PDF. Read research published in the Journal of Medicinal Chemistry Vol. 61 Issue 13 on ACS Publications, a trusted source for peer-reviewed journals., 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 …, 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 …, , Journal of Medicinal Chemistry 2001, 44, 4, 633-640 (Article) Publication Date (Web): January 12, 2001. Abstract. Full text. PDF. ABSTRACT. Read research published in the Journal of Medicinal Chemistry Vol. 44 Issue 4 on ACS Publications, a trusted source for peer-reviewed journals. , The photocaged PROTAC (phoBET1) was designed and loaded into UCNP-based mesoporous silica nanoparticles to construct a NIR light-activatable PROTAC nanocage (UMSNs@phoBET1). Under irradiation of NIR light, UMSNs@phoBET1 could be activated to achieve controllable degradation of BRD4 and on-demand antitumor therapy. View the …, Please note: If you switch to a different device, you may be asked to login again with only your ACS ID., DPP9 Comes of Age: Highly Selective Inhibitors Promise New Therapeutic Opportunities. Verónica A. Jiménez *. Journal of Medicinal Chemistry 2023, 66, 18, 12715-12716 (Viewpoint) Publication Date (Web): September 18, 2023. Abstract., 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., Tir 16, 1400 AP ... ... chemistry-related information and research through its multiple databases, peer-reviewed journals and scientific conferences. Join the ..., Farvardin 4, 1401 AP ... de Esch et al., “Fragment-to-Lead Medicinal Chemistry Publications in 2020”; J. Med. Chem. 2022. https://doi.org/10.1021/acs.jmedchem., , The emergence of resistance to PARP1 inhibitors poses a current therapeutic challenge, necessitating the development of novel strategies to overcome this …, Epub 2021 Jan 4. Author. Craig W Lindsley. PMID: 33395295. DOI: 10.1021/acs.jmedchem.0c02220. Chemistry, Pharmaceutical* Drug Discovery. …, Synthesis and biological activity of 11-Oxygenated and heterocyclic estrone analogs in pancreatic cancer monolayers and 3D spheroids. Khaled Alseud, Trevor Ostlund, Mikhail Durymanov, Joshua Reineke, Fathi Halaweish. In Press, Journal Pre-proof, Available online 5 March 2024. View PDF., 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..., This Perspective is the eighth in an annual series that summarizes successful fragment-to-lead (F2L) case studies published each year. A tabulated summary of relevant articles published in 2022 is provided, and features such as target class, screening methods, and ligand efficiency are discussed both for the 2022 examples and for the combined …, Read the latest articles of European Journal of Medicinal Chemistry at ScienceDirect.com, Elsevier’s leading platform of peer-reviewed scholarly …, Section Information. The Medicinal Chemistry Section of the journal Molecules publishes original research and review articles that increase our understanding of how the chemical structure of bioactive molecules determines their pharmacodynamic, pharmacokinetic, and physicochemical properties and, hence, their therapeutic potential. , Journal of Medicinal Chemistry 2004, 47, 7, 1605-1608 (Letter) Publication Date (Web): March 2, 2004. Abstract. Full text. PDF. ABSTRACT. Design and Synthesis of a Fluoroindolocarbazole Series as Selective Topoisomerase I Active Agents. Discovery of Water-Soluble 3,9-Difluoro-12,13-dihydro-13- [6-amino-β- d-glucopyranosyl]-5 H ,13 H …, About the Journal Journal of Medicinal Chemistry. Journal of Medicinal Chemistry. Findings on the relationship between molecular structure and biological activity or mode of action in drug discovery and development. Editor-in-Chief: Craig W. Lindsley, Vanderbilt University Medical Center. [email protected]. , Issue Publication Information. Journal of Medicinal Chemistry 2024, 67, 2, XXX-XXX (Article) Publication Date (Web): January 25, 2024. First Page. PDF. Read research published in the Journal of Medicinal Chemistry Vol. 67 Issue 2 on ACS Publications, a trusted source for peer-reviewed journals.