Search Results - "Ohwada, Jun"
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Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802)
Published in Bioorganic & medicinal chemistry (01-02-2012)“…Anaplastic lymphoma kinase (ALK) receptor tyrosine kinase is considered an attractive therapeutic target for human cancers, especially non-small cell lung…”
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Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799
Published in Bioorganic & medicinal chemistry letters (15-03-2011)“…An orally available, potent class I PI3K inhibitor, CH5132799, was discovered by structure-based drug design. Phosphatidylinositol 3-kinase (PI3K) is a lipid…”
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In vitro activity of isavuconazole against 140 reference fungal strains and 165 clinically isolated yeasts from Japan
Published in International journal of antimicrobial agents (01-10-2010)“…Abstract The in vitro susceptibilities of 140 laboratory reference strains of fungi, including type strains, and 165 clinical yeast isolates from Japan towards…”
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Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole
Published in Bioorganic & medicinal chemistry letters (01-01-2003)“…A highly potent water soluble triazole antifungal prodrug, RO0098557 ( 1), has been identified from its parent, the novel antifungal agent RO0094815 ( 2). The…”
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Synthesis of novel water soluble benzylazolium prodrugs of lipophilic azole antifungals
Published in Bioorganic & medicinal chemistry letters (07-10-2002)“…Water soluble N-benzyltriazolium or N-benzylimidazolium salt type prodrugs of several highly lipophilic triazole or imidazole antifungals have been…”
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The Selective Class I PI3K Inhibitor CH5132799 Targets Human Cancers Harboring Oncogenic PIK3CA Mutations
Published in Clinical cancer research (15-05-2011)“…The phosphatidylinositol 3-kinase (PI3K) pathway plays a central role in cell proliferation and survival in human cancer. PIK3CA mutations, which are found in…”
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9-Substituted 6,6-Dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as Highly Selective and Potent Anaplastic Lymphoma Kinase Inhibitors
Published in Journal of medicinal chemistry (22-09-2011)“…9-Substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles were discovered as highly selective and potent anaplastic lymphoma kinase (ALK) inhibitors…”
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Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability
Published in Bioorganic & medicinal chemistry (15-12-2015)“…[Display omitted] Phosphoinositide 3-kinase (PI3K) is activated in various human cancer cells and well known as a cancer therapy target. We previously reported…”
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Design and evaluation of azaindole-substituted N-hydroxypyridones as glyoxalase I inhibitors
Published in Bioorganic & medicinal chemistry letters (15-12-2012)“…We conducted a high throughput screening for glyoxalase I (GLO1) inhibitors and identified 4,6-diphenyl-N-hydroxypyridone as a lead compound. Using a binding…”
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Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents
Published in Bioorganic & medicinal chemistry (01-07-2016)“…[Display omitted] Phosphoinositide 3-kinase (PI3K) is a promising anti-cancer target, because various mutations and amplifications are observed in human tumors…”
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Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation
Published in Bioorganic & medicinal chemistry letters (01-02-2013)“…Based on structure–activity relationship information and a FlexSIS docking simulation score, aminopyrimidine was identified as a bioisostere of metabolically…”
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Abstract B157: Selective class I PI3K inhibitor CH5132799 induces significant tumor regression with suppressing 4E-BP1 phosphorylation
Published in Molecular cancer therapeutics (12-11-2011)“…Abstract The phosphatidylinositol 3-kinase (PI3K) pathway plays a central role in cell proliferation and survival in human cancer. Mutations of the PIK3CA…”
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SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF A NOVEL ANTIFUNGAL AGENT, AZOXYBACILIN
Published in Chemical & pharmaceutical bulletin (1994)“…A new antifungal substance, azoxybacilin (an unusual amino acid with an azoxy moiety) and its derivatives have been synthesized from Boc-L-Asp-OtBu utilizing…”
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Abstract 3593: Generation of a potent and selective inhibitor of ALK, CH5424802, showing superior oral bioavailability, PK profile and in vivo efficacy
Published in Cancer research (Chicago, Ill.) (15-04-2011)“…Abstract Anaplastic lymphoma kinase (ALK) is a tyrosine kinase that is constitutively activated in some cancers, due to gene alterations such as chromosomal…”
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water soluble prodrug of a novel camptothecin analog is efficacious against breast cancer resistance protein-expressing tumor xenografts
Published in Cancer chemotherapy and pharmacology (2010)“…Purpose Identification of a novel topoisomerase I inhibitor which shows superior efficacy and less individual variation than irinotecan hydrochloride (CPT-11)…”
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Synthesis of new camptothecin analogs with improved antitumor activities
Published in Bioorganic & medicinal chemistry letters (01-04-2009)“…Novel hexacyclic camptothecin analogs containing cyclic amidine, urea, or thiourea moiety were designed and synthesized based on the proposed 3D-structure of…”
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Synthesis and biological activities of a pH-dependently activated water-soluble prodrug of a novel hexacyclic camptothecin analog
Published in Bioorganic & medicinal chemistry letters (15-05-2009)“…A pH-dependently activated water-soluble antitumor prodrug, CH4556300 (TP300, a hydrochloride), was designed and synthesized from a novel hexacyclic…”
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