Current insights into anti-HIV drug discovery and development: a review of recent patent literature (2014–2017)

Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement

(2017) Xiao Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Investigational HIV integrase inhibitors in phase I and phase II clinical trials

(2017) Yingshan Han et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Identification of spirocyclic or phosphate substituted quinolizine derivatives as novel HIV-1 integrase inhibitors: a patent evaluation of WO2016094197A1, WO2016094198A1 and WO2016154527A1

(2017) Xiqiang Cheng et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Novel fused pyrimidine and isoquinoline derivatives as potent HIV-1 NNRTIs: a patent evaluation of WO2016105532A1, WO2016105534A1 and WO2016105564A1

(2017) Dongwei Kang et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Computational scaffold hopping: cornerstone for the future of drug design?

(2017) Jürgen Bajorath   Future Medicinal Chemistry

Prevalence of gag mutations associated with in vitro resistance to capsid inhibitor GS-CA1 in HIV-1 antiretroviral-naive patients

(2017) Marine Perrier et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Inhibitors of Influenza Virus Polymerase Acidic (PA) Endonuclease: Contemporary Developments and Perspectives

(2017) Han Ju et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Strategies to diversify natural products for drug discovery

(2017) Gang Li et al.   MEDICINAL RESEARCH REVIEWS

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

New Drugs in the Pipeline for the Treatment of HIV: a Review

(2017) Leigh Anne Hylton Gravatt et al.   Current Infectious Disease Reports

Identification and Characterization of BMS-955176, a Second-Generation HIV-1 Maturation Inhibitor with Improved Potency, Antiviral Spectrum, and Gag Polymorphic Coverage

(2016) Beata Nowicka-Sans et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

HIV Capsid Assembly, Mechanism, and Structure

(2016) Bo Chen   BIOCHEMISTRY

Inhibitors of HIV-1 maturation: Development of structure–activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids

(2016) Jacob J. Swidorski et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Abstract CT028: First-in-human phase I study of the nucleotide analogue NUC-3373 designed to overcome fluoropyrimidine drug resistance mechanisms

(2016) Sarah P. Blagden et al.   CANCER RESEARCH

Isoxazolidine: A Privileged Scaffold for Organic and Medicinal Chemistry

(2016) Mathéo Berthet et al.   CHEMICAL REVIEWS

The ProTides Boom

(2016) Youcef Mehellou   ChemMedChem

Discovery of bioactive molecules from CuAAC click-chemistry-based combinatorial libraries

(2016) Xueshun Wang et al.   DRUG DISCOVERY TODAY

Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket

(2016) Jiapei Yang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of non-peptide small molecular CXCR4 antagonists as anti-HIV agents: Recent advances and future opportunities

(2016) Heng Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel anti-HIV agents via Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry-based approach

(2016) Ping Gao et al.   Expert Opinion on Drug Discovery

Substituted indoles as HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent evaluation (WO2015044928)

(2016) Xiao Li et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Pyrazolo[1,5-a]pyrimidine-based macrocycles as novel HIV-1 inhibitors: a patent evaluation of WO2015123182

(2016) Lin Sun et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Novel diaryltriazines with a picolinonitrile moiety as potent HIV-1 RT inhibitors: a patent evaluation of WO2016059647(A2)

(2016) Boshi Huang et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

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

Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1

(2016) Yu Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nucleoside Phosphate and Phosphonate Prodrug Clinical Candidates

(2016) Peter J. Thornton et al.   JOURNAL OF MEDICINAL CHEMISTRY

Natural Products as Sources of New Drugs from 1981 to 2014

(2016) David J. Newman et al.   JOURNAL OF NATURAL PRODUCTS

ADMET Evaluation in Drug Discovery. 16. Predicting hERG Blockers by Combining Multiple Pharmacophores and Machine Learning Approaches

(2016) Shuangquan Wang et al.   MOLECULAR PHARMACEUTICS

Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity

(2016) Alicia Regueiro-Ren et al.   ACS Medicinal Chemistry Letters

DNA-encoded chemical libraries of macrocycles

(2015) William H Connors et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

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

Fragment-based approaches to anti-HIV drug discovery: state of the art and future opportunities

(2015) Boshi Huang et al.   Expert Opinion on Drug Discovery

Novel fluorine-containing DAPY derivatives as potent HIV-1 NNRTIs: a patent evaluation of WO2014072419

(2015) Qing Meng et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

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

HIV-1 integrase inhibition: looking at cofactor interactions

(2015) Frauke Christ et al.   Future Medicinal Chemistry

Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators

(2015) Peng Zhan 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

HIV-1 capsid: the multifaceted key player in HIV-1 infection

(2015) Edward M. Campbell et al.   NATURE REVIEWS MICROBIOLOGY

Long lasting control of viral rebound with a new drug ABX464 targeting Rev – mediated viral RNA biogenesis

(2015) Noëlie Campos et al.   Retrovirology

ABX464: a good drug candidate instead of a magic bullet

(2015) Ben Berkhout et al.   Retrovirology

Beware of docking!

(2015) Yu-Chian Chen   TRENDS IN PHARMACOLOGICAL SCIENCES

Preclinical Profile of BI 224436, a Novel HIV-1 Non-Catalytic-Site Integrase Inhibitor

(2014) Craig Fenwick et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: Design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives

(2014) Ye Tian et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis of Nucleoside Phosphate and Phosphonate Prodrugs

(2014) Ugo Pradere et al.   CHEMICAL REVIEWS

Discovery of MK-8970: An Acetal Carbonate Prodrug of Raltegravir with Enhanced Colonic Absorption

(2014) Abbas M. Walji et al.   ChemMedChem

“Old Friends in New Guise”: Exploiting Privileged Structures for Scaffold Re-Evolution/Refining

(2014) Yu'ning Song et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2: Discovery of novel [1,2,4]Triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach

(2014) Liu Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel diarylpyrimidines as potent HIV NNRTIs via a structure-guided core-refining approach

(2014) Xiao Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent review (2011 – 2014)

(2014) Xiao Li et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

LEDGINs, non-catalytic site inhibitors of HIV-1 integrase: a patent review (2006 – 2014)

(2014) Jonas Demeulemeester et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Exploring the Influence of the Protein Environment on Metal-Binding Pharmacophores

(2014) David P. Martin et al.   JOURNAL OF MEDICINAL CHEMISTRY

“Old Dogs with New Tricks”: exploiting alternative mechanisms of action and new drug design strategies for clinically validated HIV targets

(2014) Dongwei Kang et al.   Molecular BioSystems

Roles of HIV-1 capsid in viral replication and immune evasion

(2014) Valerie Le Sage et al.   VIRUS RESEARCH

Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1

(2014) Lee D. Fader et al.   ACS Medicinal Chemistry Letters

Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs

(2013) Lingzi Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Recent Advances in the Discovery and Development of Novel HIV-1 NNRTI Platforms (Part II): 2009-2013 Update#

(2013) Yu’ning Song et al.   CURRENT MEDICINAL CHEMISTRY

Emerging strategies to deplete the HIV reservoir

(2013) Nancie M. Archin et al.   CURRENT OPINION IN INFECTIOUS DISEASES

Heterocycle-thioacetic Acid Motif: A Privileged Molecular Scaffold with Potent, Broad-Ranging Pharmacological Activities

(2013) Yu’ning Song et al.   CURRENT PHARMACEUTICAL DESIGN

The A128T Resistance Mutation Reveals Aberrant Protein Multimerization as the Primary Mechanism of Action of Allosteric HIV-1 Integrase Inhibitors

(2013) Lei Feng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Macrocyclic Drugs and Clinical Candidates: What Can Medicinal Chemists Learn from Their Properties?

(2013) Fabrizio Giordanetto et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent Progress in Understanding Activity Cliffs and Their Utility in Medicinal Chemistry

(2013) Dagmar Stumpfe et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antivirals: Past, present and future

(2012) Erik De Clercq   BIOCHEMICAL PHARMACOLOGY

Targeting Protein-Protein Interactions: A Promising Avenue of Anti-HIV Drug Discovery

(2012) Peng Zhan et al.   CURRENT MEDICINAL CHEMISTRY

Recent Advances in DAPYs and Related Analogues as HIV-1 NNRTIs

(2012) Xuwang Chen et al.   CURRENT MEDICINAL CHEMISTRY

Natural Products As Sources of New Drugs over the 30 Years from 1981 to 2010

(2012) David J. Newman et al.   JOURNAL OF NATURAL PRODUCTS

Classification of scaffold-hopping approaches

(2011) Hongmao Sun et al.   DRUG DISCOVERY TODAY

Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent review (2005 – 2010)

(2011) Peng Zhan et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

1,3,4-Oxadiazole: A Privileged Structure in Antiviral Agents

(2011) Z. Li et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Probing the links between in vitro potency, ADMET and physicochemical parameters

(2011) M. Paul Gleeson et al.   NATURE REVIEWS DRUG DISCOVERY

Triterpene derivatives that inhibit human immunodeficiency virus type 1 replication

(2010) Casey R. Dorr et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Blocking Nuclear Import of Pre-Integration Complex: An Emerging Anti-HIV-1 Drug Discovery Paradigm

(2010) Peng Zhan et al.   CURRENT MEDICINAL CHEMISTRY

Privileged scaffolds for library design and drug discovery

(2010) Matthew E Welsch et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication

(2010) Frauke Christ et al.   Nature Chemical Biology