Discovery of Novel Dihydrothiopyrano[4,3-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs with Significantly Reduced hERG Inhibitory Activity and Improved Resistance Profiles

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