2021-08-12 |
Xanthine derivatives reveal an allosteric binding site in methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) |
Journal of Medicinal Chemistry. 2021 Aug 12;64(15):11288-11301. |
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2021-08-01 |
DBPR108, a novel dipeptidyl peptidase-4 inhibitor with antihyperglycemic activity |
Life Sciences. 2021 Aug 1;278:Article number 119574. |
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2021-01 |
Potent and orally active purine-based fetal hemoglobin inducers for treating Beta-thalassemia and sickle cell disease |
European Journal of Medicinal Chemistry. 2021 Jan;209:Article number 112938. |
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2019-12 |
Identification of a multitargeted tyrosine kinase inhibitor for the treatment of gastrointestinal stromal tumors and acute myeloid leukemia |
Journal of Medicinal Chemistry. 2019 Dec;62(24):11135-11150. |
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2019-05-28 |
Identification of novel anti-liver cancer small molecules with better therapeutic index than sorafenib via zebrafish drug screening platform |
Cancers. 2019 May 28;11(6):Article number 739. |
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2019-04-10 |
Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants |
Journal of Medicinal Chemistry. 2019 Apr 10;62(8):3940-3957. |
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2018-08-24 |
BPR1J373, a novel multitargeted kinase inhibitor, effectively suppresses the growth of gastrointestinal stromal tumor |
Cancer Science. 2018 Nov;109(11):3591-3601. |
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2016-10 |
BPR1J373, an oral multiple tyrosine kinase inhibitor, targets c-KIT for the treatment of c-KIT driven myeloid leukemia |
Molecular Cancer Therapeutics. 2016 Oct;15(10):2323-2333. |
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2016-04-12 |
Pyrazolylamine derivatives reveal the conformational switching between type I and type II binding modes of Anaplastic Lymphoma Kinase (ALK) |
Journal of Medicinal Chemistry. 2016 Apr 12;59(8):3906-3919. |
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2015-07 |
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations |
European Journal of Medicinal Chemistry. 2015 Jul;100:151-161. |
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2014-02 |
Fibroblast activation protein (FAP) is essential for the migration of bone marrow mesenchymal stem cells through RhoA activation |
PLoS ONE. 2014 Feb 13;9(2):Article number e88772. |
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2014-01-08 |
Evaluation of the antitumor effects of BPR1J-340, a potent and selective FLT3 inhibitor, alone or in combination with an HDAC inhibitor, vorinostat, in AML cancer |
PLoS ONE. 2014 Jan 8;9(1):Article number e83160. |
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2014-01 |
A novel dengue virus inhibitor, BP13944, discovered by high-throughput screening with dengue virus replicon cells selects for resistance in the viral NS2B/NS3 protease |
Antimicrobial Agents and Chemotherapy. 2014 Jan;58(1):110-119. |
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2013-06-28 |
Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine aurora kinase inhibitor |
Journal of Medicinal Chemistry. 2013 Jun 28;56(13):5247-5260. |
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2013-06 |
Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3) |
Bioorganic and Medicinal Chemistry. 2013 Jun;21(11):2856-2867. |
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2013-02 |
Resistance studies of a di-thiazol analogue, DBPR110, as a potential hepatitis C virus NS5A inhibitor in replicon systems |
Antimicrobial Agents and Chemotherapy. 2013 Feb; 57(2):723-733. |
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2012-06-07 |
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3) |
Bioorganic and Medicinal Chemistry Letters. 2012 Jun 7;22(14):4654-4659. |
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2012-01 |
Resistance analysis and characterization of a thiazole analogue, BP008, as a potent hepatitis C virus NS5A inhibitor |
Antimicrobial Agents and Chemotherapy. 2012 Jan;56(1):44-53. |
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2012-01 |
BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML |
British Journal of Cancer. 2012 Jan;106(3):475-481. |
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2011-07 |
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3) |
Bioorganic and Medicinal Chemistry. 2011 Jul;19(14):4173-4182 . |
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2011-06 |
Current advances and therapeutic potential of agents targeting dipeptidyl peptidases-IV, -II, 8/9 and fibroblast activation protein |
Current Topics In Medicinal Chemistry. 2011 Jun;(11):1447-1463. |
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2011-06 |
Cleavage-site specificity of prolyl endopeptidase FAP investigated with a full-length protein substrate |
Journal of Biochemistry. 2011 Jun;149(6):685-692. |
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2011-02 |
Synthesis of 3,3-dimethylglutamic acid derivatives as DPP-IV inhibitors and evaluation of their chemical stability |
Journal of the Chinese Chemical Society. 2011 Feb;58(1):108-117. |
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2010-09 |
The dimeric transmembrane domain of prolyl dipeptidase DPP-IV contributes to its quaternary structure and enzymatic activities |
Protein Science. 2010 Sep;19(9):1627-1638. |
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2010-08 |
Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein |
Journal of Medicinal Chemistry. 2010 Aug;53(18):6572-6583. |
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2010-06-15 |
(2S,4S)-1-[2-(1,1-Dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: A potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV |
Bioorganic and Medicinal Chemistry Letters. 2010 Jun 15;20(12):3596-3600. |
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2009-10 |
(1,3-Diphenyl-1H-pyrazol-4-yl)-methylamine analogues as inhibitors of dipeptidyl peptidases |
Journal of the Chinese Chemical Society. 2009 Oct;56(5):1048-1055. |
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2009-07-15 |
Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor |
Biochemical Pharmacology. 2009 Jul 15;78(2):203-210. |
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2009-06 |
A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitiors [Erratum: European Journal of Medicinal Chemistry. 2008 Aug;43(8):1603-1611.] |
European Journal of Medicinal Chemistry. 2009 Jun;44(6):2763-2763. |
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2009-04-01 |
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors |
Bioorganic and Medicinal Chemistry Letters. 2009 Apr 1;19(7):1908-1912. |
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2009-03-15 |
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors |
Bioorganic and Medicinal Chemistry. 2009 Mar 15;17(6):2388-2399. |
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2008-08 |
A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors |
European Journal of Medicinal Chemistry. 2008 Aug;43(8):1603-1611. |
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2007-03-01 |
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 |
Bioorganic and Medicinal Chemistry Letters. 2007 Mar;17(5):1274-1279. |
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2006-06-15 |
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors |
Bioorganic and Medicinal Chemistry Letters. 2006 Jun;16(12):3268-3272. |
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2006-01-12 |
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 |
Journal of Medicinal Chemistry. 2006 Jan;49(1):373-380. |
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2005-07-01 |
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors |
Bioorganic and Medicinal Chemistry Letters. 2005 Jul;15(13):3271-3275. |
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2005-04-15 |
Benzothiazolium compounds: Novel classes of inhibitors that suppress the nitric oxide production in RAW264.7 cells stimulated by LPS/IFN gamma |
Bioorganic and Medicinal Chemistry Letters. 2005 Apr;15(8):2027-2032. |
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2005-02-01 |
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8 |
Bioorganic and Medicinal Chemistry Letters. 2005 Feb;15(3):687-691. |
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