Hypoxia-inducible factor-1 (HIF-1) inhibitors from the last decade (2007 to 2016): A “structure-activity relationship” perspective

Identification of Targets of the HIF-1 Inhibitor IDF-11774 Using Alkyne-Conjugated Photoaffinity Probes

(2016) Hyun Seung Ban et al.   BIOCONJUGATE CHEMISTRY

Synthesis and biological evaluation of 1,2-dithiol-3-thiones and pyrrolo[1,2-a]pyrazines as novel hypoxia inducible factor-1 (HIF-1) inhibitor

(2016) Young Hun Lee et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and biological evaluation of C-ring truncated deguelin derivatives as heat shock protein 90 (HSP90) inhibitors

(2016) Ho Shin Kim et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Development of 1-aryl-3-furanyl/thienyl-imidazopyridine templates for inhibitors against hypoxia inducible factor (HIF)-1 transcriptional activity

(2016) Shinichiro Fuse et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

SYP-5, a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis

(2016) Li-Hui Wang et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Hypoxia-inducible factor (HIF) inhibitors: a patent survey (2011-2015)

(2016) Hyun Seung Ban et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Discovery of Manassantin A Protein Targets Using Large-Scale Protein Folding and Stability Measurements

(2016) M. Ariel Geer Wallace et al.   JOURNAL OF PROTEOME RESEARCH

Solution-phase synthesis and biological evaluation of triostin A and its analogues

(2016) Kozo Hattori et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Therapeutic targeting of hypoxia and hypoxia-inducible factors in cancer

(2016) Caroline Wigerup et al.   PHARMACOLOGY & THERAPEUTICS

LXY6090 – a novel manassantin A derivative – limits breast cancer growth through hypoxia-inducible factor-1 inhibition

(2016) Fangfang Lai et al.   OncoTargets and Therapy

A Novel Malate Dehydrogenase 2 Inhibitor Suppresses Hypoxia-Inducible Factor-1 by Regulating Mitochondrial Respiration

(2016) Hyun Seung Ban et al.   PLoS One

Chemical biology approach for the development of hypoxia inducible factor (HIF) inhibitor LW6 as a potential anticancer agent

(2015) Ravi Naik et al.   ARCHIVES OF PHARMACAL RESEARCH

HIF-1α suppressing small molecule, LW6, inhibits cancer cell growth by binding to calcineurin b homologous protein 1

(2015) Beom Seok Kim et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Design, synthesis, and structure–activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors

(2015) Yorinobu Yasuda et al.   BIOORGANIC & MEDICINAL CHEMISTRY

ortho-Carboranylphenoxyacetanilides as inhibitors of hypoxia-inducible factor (HIF)-1 transcriptional activity and heat shock protein (HSP) 60 chaperon activity

(2015) Guangzhe Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel chalcone derivatives as hypoxia-inducible factor (HIF)-1 inhibitor: Synthesis, anti-invasive and anti-angiogenic properties

(2015) Lihui Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Ring-truncated deguelin derivatives as potent Hypoxia Inducible Factor-1α (HIF-1α) inhibitors

(2015) Ho Shin Kim et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Bioactive benzofuran derivatives: Moracins A–Z in medicinal chemistry

(2015) Ravi Naik et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Biological Evaluation of Manassantin Analogues for Hypoxia-Inducible Factor 1α Inhibition

(2015) Do-Yeon Kwon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of meta -carborane-containing phenoxyacetanilides as inhibitors of hypoxia-inducible factor (HIF)-1 transcriptional activity

(2015) Guangzhe Li et al.   JOURNAL OF ORGANOMETALLIC CHEMISTRY

X609, a novel manassantin A derivative, exhibits antitumor activity in MG-63 human osteosarcoma cells in vitro and in vivo

(2015) JI LI et al.   Molecular Medicine Reports

Novel potent HIF-1 inhibitors for the prevention of tumor metastasis: discovery and optimization of 3-aryl-5-indazole-1,2,4-oxadiazole derivatives

(2015) Rong Sheng et al.   RSC Advances

HIF-1α pathway: role, regulation and intervention for cancer therapy

(2015) Georgina N. Masoud et al.   Acta Pharmaceutica Sinica B

Synthesis and structure–activity relationships of novel, potent, orally active hypoxia-inducible factor-1 inhibitors

(2014) Satoshi Nagao et al.   BIOORGANIC & MEDICINAL CHEMISTRY

HIF-1 Signaling in Drug Resistance to Chemotherapy

(2014) N.A. Warfel et al.   CURRENT MEDICINAL CHEMISTRY

Development of a Novel Class of Mitochondrial Ubiquinol–Cytochrome c Reductase Binding Protein (UQCRB) Modulators as Promising Antiangiogenic Leads

(2014) Hye Jin Jung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Structure–Activity Relationship Study of Chemical Probes as Hypoxia Induced Factor-1α/Malate Dehydrogenase 2 Inhibitors

(2014) Ravi Naik et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Synthetic Manassantin A Derivative Inhibits Hypoxia-Inducible Factor 1 and Tumor Growth

(2014) Liwei Lang et al.   PLoS One

Tetracycline analogues with a selective inhibitory effect on HIF-1α

(2014) Y. Bendiabdellah et al.   MedChemComm

Identification of Malate Dehydrogenase 2 as a Target Protein of the HIF-1 Inhibitor LW6 using Chemical Probes

(2013) Kyeong Lee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Diaryl-substituted ortho-carboranes as a new class of hypoxia inducible factor-1α inhibitors

(2013) Hiroyuki Nakamura et al.   DALTON TRANSACTIONS

Synthesis and biological evaluation of ortho-carborane containing benzoxazole as an inhibitor of hypoxia inducible factor (HIF)-1 transcriptional activity

(2013) Hiroyuki Nakamura et al.   JOURNAL OF ORGANOMETALLIC CHEMISTRY

A Cyclic Peptide Inhibitor of HIF-1 Heterodimerization That Inhibits Hypoxia Signaling in Cancer Cells

(2013) Elena Miranda et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors

(2013) Hidemitsu Minegishi et al.   ACS Medicinal Chemistry Letters

Structure–activity relationship of 2,2-dimethyl-2H-chromene based arylsulfonamide analogs of 3,4-dimethoxy-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]-N-phenylbenzenesulfonamide, a novel small molecule hypoxia inducible factor-1 (HIF-1) pathway inhibitor and anti-cancer agent

(2012) Jiyoung Mun et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Development of hypoxia-inducible factor (HIF)-1α inhibitors: Effect of ortho-carborane substituents on HIF transcriptional activity under hypoxia

(2012) Hiroyuki Nakamura et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and Biological Evaluation of Diaryl-Substituted Carboranes as Inhibitors of Hypoxia Inducible Factor (HIF)-1 Transcriptional Activity

(2012) Hidemitsu Minegishi et al.   ChemMedChem

Arylsulfonamide KCN1 Inhibits In Vivo Glioma Growth and Interferes with HIF Signaling by Disrupting HIF-1  Interaction with Cofactors p300/CBP

(2012) S. Yin et al.   CLINICAL CANCER RESEARCH

Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors

(2012) Yan Xia et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Small-molecule inhibitors of the HIF pathway and synthetic lethal interactions

(2012) Dylan T Jones et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Synthesis and Structure–Activity Relationship of (E)-Phenoxyacrylic Amide Derivatives as Hypoxia-Inducible Factor (HIF) 1α Inhibitors

(2012) Ravi Naik et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Evaluation of Novel Deguelin-Based Heat Shock Protein 90 (HSP90) Inhibitors Targeting Proliferation and Angiogenesis

(2012) Dong-Jo Chang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and in Vitro Activities of N-Alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, Novel, Small-Molecule Hypoxia Inducible Factor-1 Pathway Inhibitors and Anticancer Agents

(2012) Jiyoung Mun et al.   JOURNAL OF MEDICINAL CHEMISTRY

KCN1, a Novel Synthetic Sulfonamide Anticancer Agent: In Vitro and In Vivo Anti-Pancreatic Cancer Activities and Preclinical Pharmacology

(2012) Wei Wang et al.   PLoS One

Hypoxia-inducible factors: mediators of cancer progression and targets for cancer therapy

(2012) Gregg L. Semenza   TRENDS IN PHARMACOLOGICAL SCIENCES

Synthesis and biological activity of furanylindazoles as inhibitors of hypoxia inducible factor (HIF)-1 transcriptional activity

(2012) Ayano Takeuchi et al.   MedChemComm

Binding Model for the Interaction of Anticancer Arylsulfonamides with the p300 Transcription Cofactor

(2012) Qi Shi et al.   ACS Medicinal Chemistry Letters

Design, synthesis and insight into the structure–activity relationship of 1,3-disubstituted indazoles as novel HIF-1 inhibitors

(2011) Hongchan An et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors

(2011) Wenwei Huang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors

(2011) Chalet Tan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and Biological Evaluation of 2-Aminoisonicotinic Acid Analogues as HIF-1α Inhibitors

(2011) Yan Xia et al.   BULLETIN OF THE KOREAN CHEMICAL SOCIETY

HIF-1α inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues

(2011) Yan Xia et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Hypoxia-inducible factor inhibitors: a survey of recent patented compounds (2004 – 2010)

(2011) Hyun Seung Ban et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Design and Synthesis of Novel Small-Molecule Inhibitors of the Hypoxia Inducible Factor Pathway

(2011) Suazette Reid Mooring et al.   JOURNAL OF MEDICINAL CHEMISTRY

LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1α via upregulation of VHL in a colon cancer cell line

(2010) Kyeong Lee et al.   BIOCHEMICAL PHARMACOLOGY

Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery

(2010) Nilambari Yewalkar et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1α inhibitors

(2010) Kazuki Shimizu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of a novel small molecule targeting UQCRB of mitochondrial complex III and its anti-angiogenic activity

(2010) Hye Jin Jung et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Chalcone-based inhibitors against hypoxia-inducible factor 1—Structure activity relationship studies

(2010) Balasubramanian Srinivasan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of HSP60 as a Primary Target ofo-Carboranylphenoxyacetanilide, an HIF-1α Inhibitor

(2010) Hyun Seung Ban et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A novel benzimidazole analogue inhibits the hypoxia-inducible factor (HIF)-1 pathway

(2009) Mi-Sun Won et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Analysis of HIF-1 inhibition by manassantin A and analogues with modified tetrahydrofuran configurations

(2009) Amanda C. Kasper et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1α inhibitors

(2009) Masaharu Uno et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The first total synthesis of moracin O and moracin P, and establishment of the absolute configuration of moracin O

(2009) Navneet Kaur et al.   CHEMICAL COMMUNICATIONS

Development of HIF-1 inhibitors for cancer therapy

(2009) Barbara Onnis et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Identification of small molecule compounds that inhibit the HIF-1 signaling pathway

(2009) Menghang Xia et al.   Molecular Cancer

Acriflavine inhibits HIF-1 dimerization, tumor growth, and vascularization

(2009) K. Lee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Hypoxia-Inducible Factor-1 Inhibitory Benzofurans and Chalcone-Derived Diels−Alder Adducts fromMorusSpecies

(2008) Nguyen Tien Dat et al.   JOURNAL OF NATURAL PRODUCTS

Nucleophilic Addition of Organozinc Reagents to 2-Sulfonyl Cyclic Ethers: Stereoselective Synthesis of Manassantins A and B

(2008) Hyoungsu Kim et al.   ORGANIC LETTERS