Literature DB >> 18586498

Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton.

Aya Nakagawa1, Shigeyuki Uno, Makoto Makishima, Hiroyuki Miyachi, Yuichi Hashimoto.   

Abstract

Novel non-steroidal progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton were developed and their structure-activity relationships were investigated. Among the prepared compounds, 4-(4,4-diethyl-3,4-dihydro-1,3-dioxoquinolin-2(1H)-yl)benzonitrile (DEPIQ-4CN) showed the most potent activity, with IC(50) values of 74-78nM in alkaline phosphatase activity and reporter gene assays.

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Year:  2008        PMID： 18586498     DOI： 10.1016/j.bmc.2008.05.016

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  2 in total

1.  Synthesis of new quinazolin-2,4-diones as anti-Leishmania mexicana agents.

Authors:  Eduardo Enciso; Juan I Sarmiento-Sánchez; Héctor S López-Moreno; Adrián Ochoa-Terán; Ulises Osuna-Martínez; Evangelina Beltrán-López
Journal:  Mol Divers       Date:  2016-08-16       Impact factor: 2.943

2.  I2/TBHP mediated domino synthesis of 2-(2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)-N-aryl/alkyl benzamides and evaluation of their anticancer and docking studies.

Authors:  Anil Kumar Soda; Phani Krishna C S; Sai Krishna Chilaka; Vamshi Krishna E; Sunil Misra; Sridhar Madabhushi
Journal:  RSC Adv       Date:  2022-06-06       Impact factor: 4.036
  2 in total

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