Discovery of Novel Dihydrothiopyrano[4,3-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs with Significantly Reduced hERG Inhibitory Activity and Improved Resistance Profiles
出版年份 2021 全文链接
标题
Discovery of Novel Dihydrothiopyrano[4,3-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs with Significantly Reduced hERG Inhibitory Activity and Improved Resistance Profiles
作者
关键词
-
出版物
JOURNAL OF MEDICINAL CHEMISTRY
Volume 64, Issue 18, Pages 13658-13675
出版商
American Chemical Society (ACS)
发表日期
2021-08-26
DOI
10.1021/acs.jmedchem.1c01015
参考文献
相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。- Avoiding Drug Resistance in HIV Reverse Transcriptase
- (2021) Maria E. Cilento et al. CHEMICAL REVIEWS
- Boronic acid-containing diarylpyrimidine derivatives as novel HIV-1 NNRTIs: Design, synthesis and biological evaluation
- (2021) Da Feng et al. CHINESE CHEMICAL LETTERS
- 2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies
- (2021) Dongwei Kang et al. JOURNAL OF MEDICINAL CHEMISTRY
- New techniques and strategies in drug discovery
- (2020) Jintong Du et al. CHINESE CHEMICAL LETTERS
- Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties
- (2020) Dongwei Kang et al. JOURNAL OF MEDICINAL CHEMISTRY
- Fsp3: A new parameter for drug-likeness
- (2020) Wenxiu Wei et al. DRUG DISCOVERY TODAY
- hERG toxicity assessment: Useful guidelines for drug design
- (2020) Amanda Garrido et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Four Decades of HIV/AIDS — Much Accomplished, Much to Do
- (2020) Anthony S. Fauci et al. NEW ENGLAND JOURNAL OF MEDICINE
- Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors
- (2020) Zhen Xiao et al. BIOORGANIC & MEDICINAL CHEMISTRY
- Structure of HIV-1 RT/dsRNA initiation complex prior to nucleotide incorporation
- (2019) Kalyan Das et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles
- (2019) Boshi Huang et al. JOURNAL OF MEDICINAL CHEMISTRY
- Molecular design opportunities presented by solvent‐exposed regions of target proteins
- (2019) Xiangyi Jiang et al. MEDICINAL RESEARCH REVIEWS
- A review of methods for solubility determination in biopharmaceutical drug characterization
- (2019) Ardita Veseli et al. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
- Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs
- (2019) Dongwei Kang et al. Acta Pharmaceutica Sinica B
- Clinical Pharmacokinetics and Pharmacodynamics of Etravirine: An Updated Review
- (2019) Joshua P. Havens et al. CLINICAL PHARMACOKINETICS
- Application of Fluorine- And Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of CB1 Receptor Positive Allosteric Modulators
- (2019) Sumanta Garai et al. JOURNAL OF MEDICINAL CHEMISTRY
- A Structural View on Medicinal Chemistry Strategies against Drug Resistance
- (2018) Stefano Agnello et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Cytochrome P450 Structure, Function and Clinical Significance: A Review
- (2018) Palrasu Manikandan et al. CURRENT DRUG TARGETS
- Cytochrome P450 research and The Journal of Biological Chemistry
- (2018) F. Peter Guengerich JOURNAL OF BIOLOGICAL CHEMISTRY
- Architecture of an HIV-1 reverse transcriptase initiation complex
- (2018) Kevin P. Larsen et al. NATURE
- Future of nonnucleoside reverse transcriptase inhibitors
- (2018) Nicolas Sluis-Cremer PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Structural basis for potent and broad inhibition of HIV-1 RT by thiophene[3,2-d]pyrimidine non-nucleoside inhibitors
- (2018) Yang Yang et al. eLife
- The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic
- (2018) Vigneshwaran Namasivayam et al. JOURNAL OF MEDICINAL CHEMISTRY
- Challenges and approaches in the discovery of human immunodeficiency virus type-1 non-nucleoside reverse transcriptase inhibitors
- (2018) Leandro Battini et al. MEDICINAL RESEARCH REVIEWS
- Ligand efficiency metrics in drug discovery: the pros and cons from a practical perspective
- (2017) Maria Maddalena Cavalluzzi et al. Expert Opinion on Drug Discovery
- Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants
- (2017) Dongwei Kang et al. JOURNAL OF MEDICINAL CHEMISTRY
- Development of Safe Drugs: The hERG Challenge
- (2017) Subha Kalyaanamoorthy et al. MEDICINAL RESEARCH REVIEWS
- HIV Drug Resistance — An Emerging Threat to Epidemic Control
- (2017) Chris Beyrer et al. NEW ENGLAND JOURNAL OF MEDICINE
- Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles
- (2016) Dongwei Kang et al. JOURNAL OF MEDICINAL CHEMISTRY
- Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends
- (2015) Peng Zhan et al. JOURNAL OF MEDICINAL CHEMISTRY
- In search of a treatment for HIV – current therapies and the role of non-nucleoside reverse transcriptase inhibitors (NNRTIs)
- (2012) Chevonne Reynolds et al. CHEMICAL SOCIETY REVIEWS
- HIV-1 NNRTIs: structural diversity, pharmacophore similarity, and impliations for drug design
- (2011) Peng Zhan et al. MEDICINAL RESEARCH REVIEWS
- Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success
- (2009) Frank Lovering et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structural Basis for the Improved Drug Resistance Profile of New Generation Benzophenone Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors†
- (2008) Jingshan Ren et al. JOURNAL OF MEDICINAL CHEMISTRY
- Overcoming Undesirable hERG Potency of Chemokine Receptor Antagonists Using Baseline Lipophilicity Relationships
- (2008) Igor Shamovsky et al. JOURNAL OF MEDICINAL CHEMISTRY
Find Funding. Review Successful Grants.
Explore over 25,000 new funding opportunities and over 6,000,000 successful grants.
ExploreFind the ideal target journal for your manuscript
Explore over 38,000 international journals covering a vast array of academic fields.
Search