Emiko Kawachi

Tokyo Medical and Dental University

Author Statistics

Papers

Citation

H-Index

i-10 index

Research Field

ChemInform Abstract: Polyenylidene Thiazolidine Derivatives with Retinoidal Activities.

ChemInform (1998)

Toshihiko Tashima Hiroyuki Kagechika Motonori Tsuji Hiroshi Fukasawa Emiko Kawachi

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Thiazolidine

10.1002/chin.199818256

Cite

Citations (1)

Novel Retinoidal Tropolone Derivatives. Bioisosteric Relationship of Tropolone Ring with Benzoic Acid Moiety in Retinoid Structure.

Chemical and Pharmaceutical Bulletin (2001)

Masayuki Ebisawa Kiminori Ohta Emiko Kawachi Hiroshi Fukasawa Yuichi Hashimoto

Several tropolone derivatives (4-7) were designed as novel retinoids on the assumption that the tropolone ring may mimic the benzoic acid moiety in retinoid structures, such as Am80 (2). Among the synthesized compounds, 5-[2-(5, 6, 7, 8-tetrahydro-5, 5, 8, 8-tetramethyl-2-naphthyl)ethynyl]tropolone (7a) showed moderate potency as a differentiation-inducer of HL-60 cells. The activities of the tropolones were greatly enhanced in the presence of HX630, an RXR agonist (retinoid synergist).

Tropolone

Moiety

Benzoic acid

Retinoid X receptor

10.1248/cpb.49.501

Cite

Citations (25)

ChemInform Abstract: Design and Synthesis of Novel Retinoid Synergists Having a Dibenzodiazepine Skeleton.

ChemInform (2011)

Kiminori Ohta Emiko Kawachi Koichi Shudo Hiroyuki Kagechika

Abstract Based on the structures of two potent retinoid X receptor agonists, the novel dibenzodiazepine derivatives (VI), (VIII), and (XIII), containing two diphenylamine substructures, are designed as retinoid X receptor modulator candidates and prepared by means of Pd‐catalyzed, cf.

Diphenylamine

Retinoid X receptor

Skeleton (computer programming)

10.1002/chin.201112175

Cite

Citations (0)

Development of Retinoic Acid Receptor Antagonists Bearing Trans-Sf4-Alkynyl Structure as a Linear Linker

SSRN Electronic Journal (2022)

Shuichi Mori Nozomi Tsuemoto Emiko Kawachi Chiharu Takubo Aya Tanatani

trans -Tetrafluoro- l 6 -sulfane (tetrafluorosulfanyl, SF 4 ) compounds possess unique properties, including a linear structure and high electronegativity. Here, to investigate the utility of the trans -SF 4 moiety as a structural element of bioactive compounds, we designed and synthesized novel retinoids containing a trans -SF 4 -alkynyl group as a linear linker. The radical addition reaction of aryltetrafluorosulfanyl chloride and arylethyne, followed by elimination of hydrogen chloride, afforded the target compounds 1a â€“ 1c . Cell differentiation-inducing activity assay and reporter gene assay revealed that the trans -SF 4 -alkynyl derivatives 1b and 1c exhibit antagonistic activity towards retinoid acid receptors (RARs). Docking studies indicated that the long linear linker alters the binding mode of the compounds with the RAR a ligand-binding domain.

Linker

10.2139/ssrn.4127327

Cite

Citations (0)

Dicarba-closo-dodecaboranes as a Pharmacophore. Novel Potent Retinoidal Agonists.

Chemical and Pharmaceutical Bulletin (1999)

Yasuyuki Endo Toru Iijima Hiroyuki Kagechika Kiminori Ohta Emiko Kawachi

The synthesis and biological evaluation of the dicarba-closo-dodecaborane (carborane) derivatives of retinoids are described. Retinoidal activity was examined in terms of the differentiation-inducing ability toward human promyelocytic leukemia HL-60 cells. High retinoidal activity (agonist or antagonist for the retinoid receptor RAR) requires a carboxylic acid moiety and an appropriate hydrophobic group located at a suitable position on the molecule. 4-[4-(1,2-Dicarba-closo-dodecaboran-1-yl)phenylamino]b enzoic acids and 4-[3-(1,2-dicarba-closo-dodecaboran-1-yl)phenylamino]b enzoic acids showed potent agonistic activity at concentrations of 10(-8)-10(-9) M. The results indicate that carboranes are applicable as the hydrophobic moiety of biologically active molecules.

Moiety

Carborane

Carboxamide

10.1248/cpb.47.585

Cite

Citations (51)

Retinobenzoic acids. 1. Structure-activity relationships of aromatic amides with retinoidal activity

Journal of Medicinal Chemistry (1988)

Hiroyuki Kagechika Emiko Kawachi Yuichi Hashimoto Koichi Shudo Toshiyuki Himi

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTRetinobenzoic acids. 1. Structure-activity relationships of aromatic amides with retinoidal activityHiroyuki Kagechika, Emiko Kawachi, Yuichi Hashimoto, Koichi Shudo, and Toshiyuki HimiCite this: J. Med. Chem. 1988, 31, 11, 2182–2192Publication Date (Print):November 1, 1988Publication History Published online1 May 2002Published inissue 1 November 1988https://pubs.acs.org/doi/10.1021/jm00119a021https://doi.org/10.1021/jm00119a021research-articleACS PublicationsRequest reuse permissionsArticle Views2093Altmetric-Citations199LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts

Amide

Isopropyl

Moiety

Benzoic acid

Methyl group

Structure–activity relationship

Phenyl group

10.1021/jm00119a021

Cite

Citations (236)

Development of novel lithocholic acid derivatives as vitamin D receptor agonists

Bioorganic & Medicinal Chemistry (2019)

Hiroyuki Masuno Yuko Kazui Aya Tanatani Shinya Fujii Emiko Kawachi

Lithocholic acid

Amide

10.1016/j.bmc.2019.07.003

Cite

Citations (10)

ChemInform Abstract: Retinoidal Pyrimidinecarboxylic Acids. Unexpected Diaza‐Substituent Effects in Retinobenzoic Acids.

ChemInform (2001)

Kiminori Ohta Emiko Kawachi Noriko Inoue Hiroshi Fukasawa Yuichi Hashimoto

10.1002/chin.200112222

Cite

Citations (0)

Structural development of p-carborane-based potent non-secosteroidal vitamin D analogs

Bioorganic & Medicinal Chemistry (2014)

Shinya Fujii Ryota Sekine Atsushi Kano Hiroyuki Masuno Chalermkiat Songkram

Carborane

Moiety

Lead compound

Structure–activity relationship

Methylene

10.1016/j.bmc.2014.09.020

Cite

Citations (23)

Differentiation inducers of human promyelocytic leukemia cells HL-60. Azobenzenecarboxylic acids and stilbenecarboxylic acids.

Chemical and Pharmaceutical Bulletin (1985)

Hiroyuki Kagechika Emiko Kawachi Yuichi Hashimoto Koichi Shudo

Azobenzene-4-carboxylic acid derivatives are a new type of differentiation inducers of human myelogenous leukemia cell line HL-60. Induced cells are morphologically and functionally mature granulocytes. A study of substituent effects indicated that these compounds are related to the known synthetic retinoid, tetrahydrotetramethylnaphthyl-propenylbenzoic acid.

Inducer

10.1248/cpb.33.5597

Cite

Citations (10)