Literature DB >> 18760603

Promising core structure for nuclear receptor ligands: design and synthesis of novel estrogen receptor ligands based on diphenylamine skeleton.

Kiminori Ohta1, Yuki Chiba, Takumi Ogawa, Yasuyuki Endo.   

Abstract

Novel diphenylamine-type estrogen receptor ligands were designed and synthesized, and their biological activities were evaluated by means of binding assays for estrogen receptor-alpha and -beta and cell proliferation assay using MCF-7 cells. Compounds 4f, 11b, 12c, and 8 showed moderate estrogenic activities. We propose that the diphenylamine skeleton may be a privileged structure for various nuclear receptor ligands, including RAR, RXR, and AR ligands.

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Year:  2008        PMID： 18760603     DOI： 10.1016/j.bmcl.2008.08.004

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


  9 in total

1.  (E)-2-(2,3-Dimethyl-anilino)-N'-[2-methyl-5-(prop-1-en-2-yl)cyclo-hex-2-enyl-idene]benzohydrazide.

Authors:  Mashooq A Bhat; Hatem A Abdel-Aziz; Hazem A Ghabbour; Madhukar Hemamalini; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-03-21

2.  4-(o-Tolyl-amino)-benzaldehyde.

Authors:  Li-Ying Wang; Yong-Sheng Xie; Ren-Min Wu; Hua Zuo
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-10-20

3.  Computational investigations of the binding mechanism of novel benzophenone imine inhibitors for the treatment of breast cancer.

Authors:  Amneh Shtaiwi; Rohana Adnan; Melati Khairuddean; Shafi Ullah Khan
Journal:  RSC Adv       Date:  2019-11-01       Impact factor: 4.036

4.  Copper-catalyzed intermolecular C(sp3)-H bond functionalization towards the synthesis of tertiary carbamates.

Authors:  Prasanna Kumara Chikkade; Yoichiro Kuninobu; Motomu Kanai
Journal:  Chem Sci       Date:  2015-03-23       Impact factor: 9.825

5.  Versatile routes for synthesis of diarylamines through acceptorless dehydrogenative aromatization catalysis over supported gold-palladium bimetallic nanoparticles.

Authors:  Kento Taniguchi; Xiongjie Jin; Kazuya Yamaguchi; Kyoko Nozaki; Noritaka Mizuno
Journal:  Chem Sci       Date:  2016-12-01       Impact factor: 9.825

6.  Discovery of novel oestrogen receptor α agonists and antagonists by screening a revisited privileged structure moiety for nuclear receptors.

Authors:  Takahiro Masuya; Masaki Iwamoto; Xiaohui Liu; Ayami Matsushima
Journal:  Sci Rep       Date:  2019-07-09       Impact factor: 4.379

7.  Challenging Approach to the Development of Novel Estrogen Receptor Modulators Based on the Chemical Properties of Guaiazulene.

Authors:  Kiminori Ohta; Asako Kaise; Takumi Ogawa; Yasuyuki Endo
Journal:  Int J Mol Sci       Date:  2022-01-20       Impact factor: 5.923

8.  Triaryl-substituted Schiff bases are high-affinity subtype-selective ligands for the estrogen receptor.

Authors:  Zong-Quan Liao; Chune Dong; Kathryn E Carlson; Sathish Srinivasan; Jerome C Nwachukwu; Robert W Chesnut; Abhishek Sharma; Kendall W Nettles; John A Katzenellenbogen; Hai-Bing Zhou
Journal:  J Med Chem       Date:  2014-04-07       Impact factor: 7.446

9.  Pharmacological use of a novel scaffold, anomeric N,N-diarylamino tetrahydropyran: molecular similarity search, chemocentric target profiling, and experimental evidence.

Authors:  Arramshetti Venkanna; Oh Wook Kwon; Sualiha Afzal; Cheongyun Jang; Kyo Hee Cho; Dharmendra K Yadav; Kang Kim; Hyeung-Geun Park; Kwang-Hoon Chun; Sun Yeou Kim; Mi-Hyun Kim
Journal:  Sci Rep       Date:  2017-10-02       Impact factor: 4.379
  9 in total

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