Design, synthesis, and biological evaluation of piperidinyl‐substituted [1,2,4]triazolo[1,5‐a]pyrimidine derivatives as potential anti‐HIV‐1 agents with reduced cytotoxicity

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

Identification of Dihydrofuro[3,4-d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties

(2019) Dongwei Kang et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities

(2019) Ting Xiao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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

First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain

(2018) Boshi Huang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel diarylpyrimidines as potent HIV-1 NNRTIs by investigating the chemical space of a less explored “hydrophobic channel”

(2018) Zhongxia Zhou et al.   ORGANIC & BIOMOLECULAR 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

Discovery of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the Tolerant Region I of NNIBP

(2017) Dongwei Kang et al.   ACS Medicinal Chemistry Letters

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

Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus

(2016) Na Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dithiocarbamate–thiourea hybrids useful as vaginal microbicides also show reverse transcriptase inhibition: Design, synthesis, docking and pharmacokinetic studies

(2015) Veenu Bala et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: Optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches

(2015) Boshi Huang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: Design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines

(2015) Boshi Huang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel diarylpyrimidines and diaryltriazines as potent HIV-1 NNRTIs with dramatically improved solubility: a patent evaluation of US20140378443A1

(2015) Boshi Huang et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends

(2015) Peng Zhan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ten Paths to the Discovery of Antivirally Active Nucleoside and Nucleotide Analogues

(2012) Erik De Clercq   NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS

HIV-1 NNRTIs: structural diversity, pharmacophore similarity, and impliations for drug design

(2011) Peng Zhan et al.   MEDICINAL RESEARCH REVIEWS

Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Benzyl derivatives with broad potency against resistant mutant viruses

(2010) Denis J. Kertesz et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Physicochemical Properties of the Amorphous Drug, Cast Films, and Spray Dried Powders to Predict Formulation Probability of Success for Solid Dispersions: Etravirine

(2010) Ilse Weuts et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

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

(2008) Christophe Pannecouque et al.   Nature Protocols