國家衛生研究院 NHRI:
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    日期题名關聯
    2024-10-29 DBPR116, a prodrug of BPRMU191, in combination with naltrexone as a safer opioid analgesic than morphine via peripheral administration Journal of Medicinal Chemistry. 2024 Oct 29;Article in Press.
    2024-07-17 Discovery of a mu-opioid receptor modulator that in combination with morphinan antagonists induces analgesia Cell Chemical Biology. 2024 Jul 17;Article in Press.
    2022-12-05 Benzo[b]thiophene-2-carboxamides as novel opioid receptor agonists with potent analgesic effect and reduced constipation European Journal of Medicinal Chemistry. 2022 Dec 5;243:Article number 114728.
    2022-11 Selective and antagonist-dependent µ-opioid receptor activation by the combination of 2-{[2-(6-chloro-3,4-dihydro-1(2H)-quinolinyl)-2-oxoethyl]sulfanyl}-5-phenyl-4,6-(1H,5H)-pyrimidinedione and naloxone/naltrexone Bioorganic Chemistry. 2022 Nov;128:Article number 105905.
    2022-02-05 Discovery and development of a novel N-(3-bromophenyl)-{[(phenylcarbamoyl)amino]methyl}-N-hydroxythiophene-2-carboximidamide indoleamine 2,3-dioxygenase inhibitor using knowledge-based drug design European Journal of Medicinal Chemistry. 2022 Feb 5;229:Article number 114043.
    2021-10-14 Discovery of BPR1R024, an orally active and selective CSF1R inhibitor that exhibits antitumor and immunomodulatory activity in a murine colon tumor model Journal of Medicinal Chemistry. 2021 Oct 14;64(19):14477-14497.
    2021-05-19 Discovery and synthesis of a pyrimidine-based aurora kinase inhibitor to reduce levels of MYC oncoproteins Journal of Medicinal Chemistry. 2021 May 19;64(11):7312-7330.
    2021-01 BPRDP056, a novel small molecule drug conjugate specifically targeting phosphatidylserine for cancer therapy Translational Oncology. 2021 Jan;14(1):Article number 100897.
    2020-10-08 Comparative study between deep learning and QSAR classifications for TNBC inhibitors and novel GPCR agonist discovery Scientific Reports. 2020 Oct 8;10:Article number 16771.
    2020-08 BPR6K609: An Aurora kinase inhibitor targeting small cell lung cancer with MYC amplification Cancer Research. 2020 Aug;80(16):1937.
    2020-04 BPR1M97, a dual mu opioid receptor/nociceptin-orphanin FQ peptide receptor agonist, produces potent antinociceptive effects with safer properties than morphine Neuropharmacology. 2020 Apr;166:Article number 107678.
    2020-02-10 Unique sulfur-aromatic interactions contribute to the binding of potent imidazothiazole indoleamine 2,3-Dioxygenase inhibitors Journal of Medicinal Chemistry. 2020 Feb 10;63(4):1642-1659.
    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.
    2019-10 Inhibition of Rspo-Wnt pathway facilitates checkpoint blockade therapy by anti-RSPO3 antibody (DBPR117) Annals of Oncology. 2019 Oct;30(Suppl. 5):191.
    2019-07-11 Linker optimization and therapeutic evaluation of phosphatidylserine-targeting zinc dipicolylamine-based drug conjugates Journal of Medicinal Chemistry. 2019 Jul 11;62(13):6047-6062.
    2019-07 Use of integrated genomic analyses in patient-derived tumor model to discover new clinical indications for the multikinase inhibitor drug candidate, DBPR216 Cancer Research. 2019 Jul;79(13, Suppl.):Abstract number 4626.
    2019-07 BPRDP056, a novel small molecule drug conjugate specifically targeting phosphatidylserine for cancer therapy Cancer Research. 2019 Jul;79(13, Suppl.):Abstract number 227.
    2019-07 An Aurora kinase inhibitor BPR6K471 inhibits tumor growth and reduces the cancer stem cell-like properties of small cell lung cancer Cancer Research. 2019 Jul;79(13, Suppl.):Abstract number 3851.
    2019-04-01 The in vivo antinociceptive and mu-opioid receptor activating effects of the combination of N-phenyl-2′,4′-dimethyl-4,5′-bi-1,3-thiazol-2-amines and naloxone European Journal of Medicinal Chemistry. 2019 Apr 1;167:312-323.
    2018-12 Targeting RSPO3 reduces stem cell function in RSPO3-Fusion-positive colon cancer and RSPO3 high lung cancer Cancer Science. 2018 Dec;109(SI, Suppl. 2):210.
    2018-12 Targeting RSPO3 reduces stem cell function in RSPO3-Fusion-positive colon cancer and RSPO3 high lung cancer Cancer Science. 2018 Dec;109(Suppl. 2, SI):1257.
    2018-05-10 Design and synthesis of BPR1K653 derivatives targeting the back pocket of Aurora kinases for selective isoform inhibition European Journal of Medicinal Chemistry. 2018 May 10;151:533-545.
    2018-04 4-Bromophenylhydrazinyl benzenesulfonylphenylureas as indoleamine 2,3-dioxygenase inhibitors with in vivo target inhibition and anti-tumor efficacy Bioorganic Chemistry. 2018 Apr;77:600-607.
    2017-07 Design, synthesis, and evaluation of thiazolidine-2,4-dione derivatives as a novel class of glutaminase inhibitors Journal of Medicinal Chemistry. 2017 Jul;60(13):5599-5612.
    2017-06-22 Targeting coronaviral replication and cellular JAK2 mediated dominant NF-kappaB activation for comprehensive and ultimate inhibition of coronaviral activity Scientific Reports. 2017 Jun 22;7:Article number 4105.
    2017-05 1-(2,4-Dibromophenyl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one: A novel opioid receptor agonist with less accompanying gastrointestinal dysfunction than morphine Anesthesiology. 2017 May;126(5):952-966.
    2017-01 Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists European Journal of Medicinal Chemistry. 2017 Jan;126:202-217.
    2016-12 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 Oncotarget. 2016 Dec;7(52):86239-86256.
    2016-12 Phenyl benzenesulfonylhydrazides: Selective indoleamine 2,3-dioxygenase inhibitors with potent in vivo pharmacodynamic activity and antitumor efficacy European Journal of Cancer. 2016 Dec;68(Suppl. 1):S83-S84.
    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.
    2016-01 Important hydrogen bond networks in Indoleamine 2,3-Dioxygenase 1 (IDO1) inhibitor design revealed by crystal structures of imidazoleisoindole derivatives with IDO1 Journal of Medicinal Chemistry. 2016 Jan;59 (1):282-293.
    2016-01 Phenyl benzenesulfonylhydrazides exhibit selective Indoleamine 2,3-Dioxygenase inhibition with potent in vivo pharmacodynamic activity and antitumor efficacy Journal of Medicinal Chemistry. 2016 Jan;59(1):419-430.
    2015-12 Novel oxime-bearing coumarin derivatives act as potent Nrf2/ARE activators in vitro and in mouse model European Journal of Medicinal Chemistry. 2015 Dec;106:60-74.
    2015-10 Identification of substituted naphthotriazolediones as novel tryptophan 2,3-dioxygenase (TDO) inhibitors through structure-based virtual screening Journal of Medicinal Chemistry. 2015 Oct;58 (19):7807-7819.
    2015-08 Novel Nrf2/ARE activator, trans-coniferylaldehyde, induces a HO-1-mediated defense mechanism through a dual p38alpha/MAPKAPK-2 and PK-N3 signaling pathway Chemical Research in Toxicology. 2015 Aug ;28(9):1681-1692.
    2015-08 Zinc-dipicolylamine directed pharmaceutical delivery system (ZAPS) as an innovative cancer drug delivery platform Cancer Research. 2015 Aug;75(Suppl. 15):Abstract number 4413.
    2015-06-29 Homology modeling of DFG-in FMS-like tyrosine kinase 3 (FLT3) and structure-based virtual screening for inhibitor identification Scientific Reports. 2015 Jun 29;5:Article number 11702.
    2014-09 Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists Bioorganic and Medicinal Chemistry. 2014 Sep;22(17): 4694-4703.
    2014-08 Discovery and structure-activity relationships of phenyl benzenesulfonylhydrazides as novel indoleamine 2,3-dioxygenase inhibitors Bioorganic and Medicinal Chemistry Letters. 2014 Aug;24(15):3403-3406.

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