Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs

Druggability modification strategies of the diarylpyrimidine‐type non‐nucleoside reverse transcriptase inhibitors

(2021) Li Ding et al.   MEDICINAL RESEARCH REVIEWS

Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors

(2021) Helen E. Aylott et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from N-Alkylation to Methyl Hopping on the Pyrimidine Ring

(2021) Li Ding et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ligand-based substituent-anchoring design of selective receptor-interacting protein kinase 1 necroptosis inhibitors for ulcerative colitis therapy

(2021) Jing Zhu et al.   Acta Pharmaceutica Sinica B

Pharmacophore-fusing design of pyrimidine sulfonylacetanilides as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase

(2020) Yali Sang et al.   BIOORGANIC CHEMISTRY

Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel

(2020) Dongwei Kang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design of Biphenyl-Substituted Diarylpyrimidines with a Cyanomethyl Linker as HIV-1 NNRTIs via a Molecular Hybridization Strategy

(2020) Yuan Lei et al.   MOLECULES

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

Scaffold Hopping in Discovery of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: From CH(CN)-DABOs to CH(CN)-DAPYs

(2020) Ting-Ting Li et al.   MOLECULES

Privileged scaffold inspired design of novel oxime-biphenyl-DAPYs in treatment of HIV-1

(2020) Yang Yang et al.   BIOORGANIC CHEMISTRY

Structure–Activity Relationship Exploration of NNIBP Tolerant Region I Leads to Potent HIV-1 NNRTIs

(2020) Dongwei Kang et al.   ACS Infectious Diseases

Radiosensitization of human pancreatic cancer by piperlongumine analogues

(2020) Hao Ma et al.   CHINESE CHEMICAL LETTERS

Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors

(2020) Xiaomei Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Neuroprotective Effect of Swertiamain on Cerebral Ischemia/Reperfusion Injury by Inducing the Nrf2 Protective Pathway

(2019) Hui Wang et al.   ACS Chemical Neuroscience

Follow on-based optimization of the biphenyl-DAPYs as HIV-1 nonnucleoside reverse transcriptase inhibitors against the wild-type and mutant strains

(2019) Yali Sang et al.   BIOORGANIC CHEMISTRY

Fragment-based discovery of sulfur-containing diarylbenzopyrimidines as novel nonnucleoside reverse transcriptase inhibitors

(2019) Sheng Han et al.   CHINESE CHEMICAL LETTERS

Molecular Hybridization-Inspired Optimization of Diarylbenzopyrimidines as HIV-1 Nonnucleoside Reverse Transcriptase Inhibitors with Improved Activity against K103N and E138K Mutants and Pharmacokinetic Profiles

(2019) Sheng Han et al.   ACS Infectious Diseases

Improving the positional adaptability: structure-based design of biphenyl-substituted diaryltriazines as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

(2019) Kaijun Jin et al.   Acta Pharmaceutica Sinica B

Development of non-nucleoside reverse transcriptase inhibitors (NNRTIs): Our past twenty years

(2019) Chunlin Zhuang et al.   Acta Pharmaceutica Sinica B

Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles

(2019) Yali Sang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1

(2018) KaiJun Jin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Structure–Activity Relationship (SAR) Studies of Novel Pyrazolopyridine Derivatives as Inhibitors of Enterovirus Replication

(2018) Yanpeng Xing et al.   JOURNAL OF MEDICINAL CHEMISTRY

Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors

(2018) Shuang-Xi Gu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Rapid Identification of Keap1–Nrf2 Small-Molecule Inhibitors through Structure-Based Virtual Screening and Hit-Based Substructure Search

(2014) Chunlin Zhuang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals

(2014) Edon Vitaku et al.   JOURNAL OF MEDICINAL CHEMISTRY

Mitigating Heterocycle Metabolism in Drug Discovery

(2012) David J. St. Jean et al.   JOURNAL OF MEDICINAL CHEMISTRY

Strategies and Chemical Design Approaches to Reduce the Potential for Formation of Reactive Metabolic Species

(2011) Upendra A. Argikar et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design

(2011) Nicholas A. Meanwell   JOURNAL OF MEDICINAL CHEMISTRY

Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 5. An Evolution from Indole to Azaindoles Leading to the Discovery of 1-(4-Benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a Drug Candidate That Demonstrates Antiviral Activity in HIV-1-Infected Subjects∞

(2009) Tao Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: revisited 20 years later

(2008) Christophe Pannecouque et al.   Nature Protocols