Literature DB >> 17651968

Synthesis and structure-activity relationship of novel RXR antagonists: orally active anti-diabetic and anti-obesity agents.

Junichi Sakaki1, Masashi Kishida, Kazuhide Konishi, Hiroki Gunji, Atsushi Toyao, Yuki Matsumoto, Takanori Kanazawa, Hidefumi Uchiyama, Hiroaki Fukaya, Hironobu Mitani, Yoshie Arai, Masaaki Kimura.   

Abstract

A series of diazepinylbenzoic acid derivatives were synthesized and tested in the inhibition assay of the transactivation of RXR. Oral treatment of cyano derivatives (16f) was found to show anti-diabetic and anti-obesity effects in KK-A(y) mice.

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Year:  2007        PMID： 17651968     DOI： 10.1016/j.bmcl.2007.06.080

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 in total

1.  Design, synthesis, and characterization of rhein analogs as novel inhibitors of scavenger receptor A.

Authors:  Yi Zheng; Xia Li; Piyusha P Pagare; Yunyun Yuan; Xiang-Yang Wang; Yan Zhang
Journal:  Bioorg Med Chem Lett       Date:  2016-11-12       Impact factor: 2.823

2.  Danthron functions as a retinoic X receptor antagonist by stabilizing tetramers of the receptor.

Authors:  Haitao Zhang; Rong Zhou; Li Li; Jing Chen; Lili Chen; Chenjing Li; Hong Ding; Liang Yu; Lihong Hu; Hualiang Jiang; Xu Shen
Journal:  J Biol Chem       Date:  2010-11-17       Impact factor: 5.157

3.  Modeling, synthesis and biological evaluation of potential retinoid X receptor-selective agonists: novel halogenated analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene).

Authors:  Julie K Furmick; Ichiro Kaneko; Angela N Walsh; Joanna Yang; Jaskaran S Bhogal; Geoffrey M Gray; Juan C Baso; Drew O Browder; Jessica L S Prentice; Luis A Montano; Chanh C Huynh; Lisa M Marcus; Dorian G Tsosie; Jungeun S Kwon; Alexis Quezada; Nicole M Reyes; Brittney Lemming; Puneet Saini; Arjan van der Vaart; Thomas L Groy; Pamela A Marshall; Peter W Jurutka; Carl E Wagner
Journal:  ChemMedChem       Date:  2012-09       Impact factor: 3.466

4.  Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene).

Authors:  Carl E Wagner; Peter W Jurutka; Pamela A Marshall; Thomas L Groy; Arjan van der Vaart; Joseph W Ziller; Julie K Furmick; Mark E Graeber; Erik Matro; Belinda V Miguel; Ivy T Tran; Jungeun Kwon; Jamie N Tedeschi; Shahram Moosavi; Amina Danishyar; Joshua S Philp; Reina O Khamees; Jevon N Jackson; Darci K Grupe; Syed L Badshah; Justin W Hart
Journal:  J Med Chem       Date:  2009-10-08       Impact factor: 7.446

5.  2-Fluoro-4-(meth-oxy-carbon-yl)benzoic acid.

Authors:  Carl E Wagner; Thomas L Groy
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-08-18

Review 6.  Retinoid X Receptor Antagonists.

Authors:  Masaki Watanabe; Hiroki Kakuta
Journal:  Int J Mol Sci       Date:  2018-08-10       Impact factor: 5.923

7.  Phenotypic landscape of intestinal organoid regeneration.

Authors:  Ilya Lukonin; Denise Serra; Ludivine Challet Meylan; Katrin Volkmann; Janine Baaten; Rui Zhao; Shelly Meeusen; Karyn Colman; Francisca Maurer; Michael B Stadler; Jeremy Jenkins; Prisca Liberali
Journal:  Nature       Date:  2020-10-07       Impact factor: 49.962
  7 in total

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