List of works - Hsing-Pang Hsieh

2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.

scientific article published in January 2006

2-amino-3,4,5-trimethoxybenzophenones as potent tubulin polymerization inhibitors

scientific article published on 4 January 2011

3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes

scientific article published on 12 December 2006

3D-QSAR-assisted drug design: identification of a potent quinazoline-based Aurora kinase inhibitor.

scientific article published on 22 November 2012

4- and 5-aroylindoles as novel classes of potent antitubulin agents.

scientific article published on 8 August 2007

5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors

scientific article

7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents

scientific article published on November 2006

A cell-based high-throughput screen for epidermal growth factor receptor pathway inhibitors

scientific article

A novel aurora-A inhibitor, BPR1K0609S1, sensitizes colorectal tumor cells to 5-fluorofracil (5-FU) treatment

scientific article published on 29 April 2013

A novel bis-benzylidenecyclopentanone derivative, BPR0Y007, inducing a rapid caspase activation involving upregulation of Fas (CD95/APO-1) and wild-type p53 in human oral epidermoid carcinoma cells.

scientific article

A selective Aurora-A 5'-UTR siRNA inhibits tumor growth and metastasis

scientific article published on 23 December 2019

Advances in Aurora kinase inhibitor patents

scientific article published on March 2009

An antimitotic and antivascular agent BPR0L075 overcomes multidrug resistance and induces mitotic catastrophe in paclitaxel-resistant ovarian cancer cells

scientific article

Anti-HSV activity of digitoxin and its possible mechanisms.

scientific article

Anti-influenza drug discovery: identification of an orally bioavailable quinoline derivative through activity- and property-guided lead optimization.

scientific article

Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives.

scientific article

Antiviral drug discovery against SARS-CoV.

scientific article

Aurintricarboxylic acid inhibits influenza virus neuraminidase

scientific article

Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold

scientific article

Aurora kinase inhibitor patents and agents in clinical testing: an update (2009-10).

scientific article published on June 2011

Aurora kinase inhibitors in preclinical and clinical testing

scientific article published on 01 April 2009

Aurora kinase inhibitors reveal mechanisms of HURP in nucleation of centrosomal and kinetochore microtubules

scientific article

BPR0L075, a novel synthetic indole compound with antimitotic activity in human cancer cells, exerts effective antitumoral activity in vivo.

scientific article published on July 2004

BPR1K653, a novel Aurora kinase inhibitor, exhibits potent anti-proliferative activity in MDR1 (P-gp170)-mediated multidrug-resistant cancer cells

scientific article

Biomimetic Syntheses of (±)-Isopalhinine A, (±)-Palhinine A, and (±)-Palhinine D

scientific article published on 30 October 2018

Biotransformation of 6-methoxy-3-(3',4',5'-trimethoxy-benzoyl)-1H-indole (BPR0L075), a novel antimicrotubule agent, by mouse, rat, dog, and human liver microsomes.

scientific article published on 2 April 2007

Bortezomib overcomes tumor necrosis factor-related apoptosis-inducing ligand resistance in hepatocellular carcinoma cells in part through the inhibition of the phosphatidylinositol 3-kinase/Akt pathway

scientific article published on 04 March 2009

CDKN1A-mediated responsiveness of MLL-AF4-positive acute lymphoblastic leukemia to Aurora kinase-A inhibitors.

scientific article published on 13 January 2014

Cancer Cells Acquire Mitotic Drug Resistance Properties Through Beta I-Tubulin Mutations and Alterations in the Expression of Beta-Tubulin Isotypes ⬇️

scientific article published on September 3, 2010

Combined modalities of resistance in an oxaliplatin-resistant human gastric cancer cell line with enhanced sensitivity to 5-fluorouracil.

scientific article published on 3 July 2007

Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.

scientific article published on August 2004

Delineating the active site architecture of G9a lysine methyltransferase through substrate and inhibitor binding mode analysis: a molecular dynamics study

scientific article published on 17 November 2018

Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists

scientific article

Design and synthesis of BPR1K653 derivatives targeting the back pocket of Aurora kinases for selective isoform inhibition.

scientific article published on 3 April 2018

Development and validation of a liquid chromatography-tandem mass spectrometry for the determination of BPR0L075, a novel antimicrotuble agent, in rat plasma: application to a pharmacokinetic study

scientific article published on 26 September 2006

Discovery of BPR1K871, a quinazoline based, multi-kinase inhibitor for the treatment of AML and solid tumors: Rational design, synthesis, in vitro and in vivo evaluation

scientific article

Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer

scientific article published on 15 November 2019

Discovery of a novel family of SARS-CoV protease inhibitors by virtual screening and 3D-QSAR studies

scientific article published on 01 June 2006

Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design.

scientific article published on 16 August 2016

Drug repurposing for chronic myeloid leukemia: in silico and in vitro investigation of DrugBank database for allosteric Bcr-Abl inhibitors

scientific article published on 29 June 2016

Dual Kit/Aur Inhibitors as Chemosensitizing Agents for the Treatment of Melanoma: Design, Synthesis, Docking Studies and Functional Investigation

scientific article published on 09 July 2019

Dual inhibition of topoisomerase I and tubulin polymerization by BPR0Y007, a novel cytotoxic agent.

scientific article published in June 2003

Evaluation of metal-conjugated compounds as inhibitors of 3CL protease of SARS-CoV.

scientific article published in September 2004

Facile identification of dual FLT3-Aurora A inhibitors: a computer-guided drug design approach.

scientific article published on 24 March 2014

Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification

scientific article

First total syntheses of (+/-)-annuionone B and (+/-)-tanarifuranonol

scientific article published on 04 January 2008

Generation of ligand-based pharmacophore model and virtual screening for identification of novel tubulin inhibitors with potent anticancer activity.

scientific article published in July 2009

Homology modeling of DFG-in FMS-like tyrosine kinase 3 (FLT3) and structure-based virtual screening for inhibitor identification.

scientific article published on 29 June 2015

Identification of ligand efficient, fragment-like hits from an HTS library: structure-based virtual screening and docking investigations of 2H- and 3H-pyrazolo tautomers for Aurora kinase A selectivity.

scientific article published on 26 October 2014

Identification of novel quinoline inhibitor for EHMT2/G9a through virtual screening

scientific article published on 20 November 2019

Inhibition of HIV-1 Tat-mediated transcription by a coumarin derivative, BPRHIV001, through the Akt pathway.

scientific article

Inhibition of SARS-CoV 3C-like Protease Activity by Theaflavin-3,3'-digallate (TF3)

scientific article

Inhibition of severe acute respiratory syndrome coronavirus replication by niclosamide

scientific article

Insights for the design of protein lysine methyltransferase G9a inhibitors

scientific article published on 29 May 2019

Isocostunolide, a sesquiterpene lactone, induces mitochondrial membrane depolarization and caspase-dependent apoptosis in human melanoma cells.

scientific article published on 11 May 2006

Ligand efficiency based approach for efficient virtual screening of compound libraries.

scientific article

Lysosomal cysteine protease cathepsin S is involved in cancer cell motility by regulating store-operated Ca2+ entry

scientific article published on 21 July 2019

Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities.

scientific article published on December 2005

Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine Aurora kinase inhibitor.

scientific article

Parallel screening of wild-type and drug-resistant targets for anti-resistance neuraminidase inhibitors

scientific article

Pharmaceutical design of antimitotic agents based on combretastatins.

scientific article

Pronounced induction of endoplasmic reticulum stress and tumor suppression by surfactant-free poly(lactic-co-glycolic acid) nanoparticles via modulation of the PI3K signaling pathway.

scientific article

Protein Kinase Inhibitor Design by Targeting the Asp-Phe-Gly (DFG) Motif: The Role of the DFG Motif in the Design of Epidermal Growth Factor Receptor Inhibitors ⬇️

scientific article published on May 10, 2013

Pyrazole compound BPR1P0034 with potent and selective anti-influenza virus activity

scientific article

Scaffold-hopping strategy: synthesis and biological evaluation of 5,6-fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents.

scientific article published on 24 March 2011

Small-molecule EGFR tyrosine kinase inhibitors for the treatment of cancer

scientific article

Strategies of development of antiviral agents directed against influenza virus replication

scientific article

Structural basis for the improved potency of peroxisome proliferator-activated receptor (PPAR) agonists

scientific article published on October 2010

Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.

scientific article published in January 2003

Structure-activity relationship studies of 3-aroylindoles as potent antimitotic agents.

scientific article published on October 2006

Structure-based drug design of a novel family of PPARgamma partial agonists: virtual screening, X-ray crystallography, and in vitro/in vivo biological activities.

scientific article published on May 2006

Structure-based drug design of novel Aurora kinase A inhibitors: structural basis for potency and specificity

scientific article

Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors

scientific article published on 11 April 2006

Survivin counteracts the therapeutic effect of microtubule de-stabilizers by stabilizing tubulin polymers.

scientific article published on 03 July 2009

Synthesis and anti-viral activity of a series of sesquiterpene lactones and analogues in the subgenomic HCV replicon system.

scientific article

Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents.

scientific article published on 20 May 2011

Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors

scientific article published on 9 February 2008

Synthesis and evaluation of 3-aroylindoles as anticancer agents: metabolite approach.

scientific article published in August 2009

Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.

scientific article published in June 2002

Synthesis and structure-activity relationships of 2-amino-1-aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents.

scientific article

Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents.

scientific article published on May 2004

Targeting P-glycoprotein: Investigation of piperine analogs for overcoming drug resistance in cancer.

scientific article published on 11 August 2017

Therapeutic polymeric nanoparticles and the methods of making and using thereof: a patent evaluation of WO2015036792.

scientific article

Thiopurine analogues inhibit papain-like protease of severe acute respiratory syndrome coronavirus.

scientific article published on 19 January 2008

Tubulin-destabilizing agent BPR0L075 induces vascular-disruption in human breast cancer mammary fat pad xenografts

scientific article

List of works by Hsing-Pang Hsieh

2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.

2-amino-3,4,5-trimethoxybenzophenones as potent tubulin polymerization inhibitors

3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes

3D-QSAR-assisted drug design: identification of a potent quinazoline-based Aurora kinase inhibitor.

4- and 5-aroylindoles as novel classes of potent antitubulin agents.

5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors

7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents

A cell-based high-throughput screen for epidermal growth factor receptor pathway inhibitors

A novel aurora-A inhibitor, BPR1K0609S1, sensitizes colorectal tumor cells to 5-fluorofracil (5-FU) treatment

A novel bis-benzylidenecyclopentanone derivative, BPR0Y007, inducing a rapid caspase activation involving upregulation of Fas (CD95/APO-1) and wild-type p53 in human oral epidermoid carcinoma cells.

A selective Aurora-A 5'-UTR siRNA inhibits tumor growth and metastasis

Advances in Aurora kinase inhibitor patents

An antimitotic and antivascular agent BPR0L075 overcomes multidrug resistance and induces mitotic catastrophe in paclitaxel-resistant ovarian cancer cells

Anti-HSV activity of digitoxin and its possible mechanisms.

Anti-influenza drug discovery: identification of an orally bioavailable quinoline derivative through activity- and property-guided lead optimization.

Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives.

Antiviral drug discovery against SARS-CoV.

Aurintricarboxylic acid inhibits influenza virus neuraminidase

Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold

Aurora kinase inhibitor patents and agents in clinical testing: an update (2009-10).

Aurora kinase inhibitors in preclinical and clinical testing

Aurora kinase inhibitors reveal mechanisms of HURP in nucleation of centrosomal and kinetochore microtubules

BPR0L075, a novel synthetic indole compound with antimitotic activity in human cancer cells, exerts effective antitumoral activity in vivo.

BPR1K653, a novel Aurora kinase inhibitor, exhibits potent anti-proliferative activity in MDR1 (P-gp170)-mediated multidrug-resistant cancer cells

Biomimetic Syntheses of (±)-Isopalhinine A, (±)-Palhinine A, and (±)-Palhinine D

Biotransformation of 6-methoxy-3-(3',4',5'-trimethoxy-benzoyl)-1H-indole (BPR0L075), a novel antimicrotubule agent, by mouse, rat, dog, and human liver microsomes.

Bortezomib overcomes tumor necrosis factor-related apoptosis-inducing ligand resistance in hepatocellular carcinoma cells in part through the inhibition of the phosphatidylinositol 3-kinase/Akt pathway

CDKN1A-mediated responsiveness of MLL-AF4-positive acute lymphoblastic leukemia to Aurora kinase-A inhibitors.

Cancer Cells Acquire Mitotic Drug Resistance Properties Through Beta I-Tubulin Mutations and Alterations in the Expression of Beta-Tubulin Isotypes ⬇️

Combined modalities of resistance in an oxaliplatin-resistant human gastric cancer cell line with enhanced sensitivity to 5-fluorouracil.

Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.

Delineating the active site architecture of G9a lysine methyltransferase through substrate and inhibitor binding mode analysis: a molecular dynamics study

Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists

Design and synthesis of BPR1K653 derivatives targeting the back pocket of Aurora kinases for selective isoform inhibition.

Development and validation of a liquid chromatography-tandem mass spectrometry for the determination of BPR0L075, a novel antimicrotuble agent, in rat plasma: application to a pharmacokinetic study

Discovery of BPR1K871, a quinazoline based, multi-kinase inhibitor for the treatment of AML and solid tumors: Rational design, synthesis, in vitro and in vivo evaluation

Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer

Discovery of a novel family of SARS-CoV protease inhibitors by virtual screening and 3D-QSAR studies

Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design.

Drug repurposing for chronic myeloid leukemia: in silico and in vitro investigation of DrugBank database for allosteric Bcr-Abl inhibitors

Dual Kit/Aur Inhibitors as Chemosensitizing Agents for the Treatment of Melanoma: Design, Synthesis, Docking Studies and Functional Investigation

Dual inhibition of topoisomerase I and tubulin polymerization by BPR0Y007, a novel cytotoxic agent.

Evaluation of metal-conjugated compounds as inhibitors of 3CL protease of SARS-CoV.

Facile identification of dual FLT3-Aurora A inhibitors: a computer-guided drug design approach.

Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification

First total syntheses of (+/-)-annuionone B and (+/-)-tanarifuranonol

Generation of ligand-based pharmacophore model and virtual screening for identification of novel tubulin inhibitors with potent anticancer activity.

Homology modeling of DFG-in FMS-like tyrosine kinase 3 (FLT3) and structure-based virtual screening for inhibitor identification.

Identification of ligand efficient, fragment-like hits from an HTS library: structure-based virtual screening and docking investigations of 2H- and 3H-pyrazolo tautomers for Aurora kinase A selectivity.

Identification of novel quinoline inhibitor for EHMT2/G9a through virtual screening

Inhibition of HIV-1 Tat-mediated transcription by a coumarin derivative, BPRHIV001, through the Akt pathway.

Inhibition of SARS-CoV 3C-like Protease Activity by Theaflavin-3,3'-digallate (TF3)

Inhibition of severe acute respiratory syndrome coronavirus replication by niclosamide

Insights for the design of protein lysine methyltransferase G9a inhibitors

Isocostunolide, a sesquiterpene lactone, induces mitochondrial membrane depolarization and caspase-dependent apoptosis in human melanoma cells.

Ligand efficiency based approach for efficient virtual screening of compound libraries.

Lysosomal cysteine protease cathepsin S is involved in cancer cell motility by regulating store-operated Ca2+ entry

Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities.

Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine Aurora kinase inhibitor.

Parallel screening of wild-type and drug-resistant targets for anti-resistance neuraminidase inhibitors

Pharmaceutical design of antimitotic agents based on combretastatins.

Pronounced induction of endoplasmic reticulum stress and tumor suppression by surfactant-free poly(lactic-co-glycolic acid) nanoparticles via modulation of the PI3K signaling pathway.

Protein Kinase Inhibitor Design by Targeting the Asp-Phe-Gly (DFG) Motif: The Role of the DFG Motif in the Design of Epidermal Growth Factor Receptor Inhibitors ⬇️

Pyrazole compound BPR1P0034 with potent and selective anti-influenza virus activity

Scaffold-hopping strategy: synthesis and biological evaluation of 5,6-fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents.

Small-molecule EGFR tyrosine kinase inhibitors for the treatment of cancer

Strategies of development of antiviral agents directed against influenza virus replication

Structural basis for the improved potency of peroxisome proliferator-activated receptor (PPAR) agonists

Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.

Structure-activity relationship studies of 3-aroylindoles as potent antimitotic agents.

Structure-based drug design of a novel family of PPARgamma partial agonists: virtual screening, X-ray crystallography, and in vitro/in vivo biological activities.

Structure-based drug design of novel Aurora kinase A inhibitors: structural basis for potency and specificity

Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors

Survivin counteracts the therapeutic effect of microtubule de-stabilizers by stabilizing tubulin polymers.

Synthesis and anti-viral activity of a series of sesquiterpene lactones and analogues in the subgenomic HCV replicon system.

Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents.

Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors

Synthesis and evaluation of 3-aroylindoles as anticancer agents: metabolite approach.

Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.