Literature DB >> 20172725

Discovery and SAR of hydantoin TACE inhibitors.

Wensheng Yu1, Zhuyan Guo, Peter Orth, Vincent Madison, Lei Chen, Chaoyang Dai, Robert J Feltz, Vinay M Girijavallabhan, Seong Heon Kim, Joseph A Kozlowski, Brian J Lavey, Dansu Li, Daniel Lundell, Xiaoda Niu, John J Piwinski, Janeta Popovici-Muller, Razia Rizvi, Kristin E Rosner, Bandarpalle B Shankar, Neng-Yang Shih, M Arshad Siddiqui, Jing Sun, Ling Tong, Shelby Umland, Michael K C Wong, De-yi Yang, Guowei Zhou.   

Abstract

We disclose inhibitors of TNF-alpha converting enzyme (TACE) designed around a hydantoin zinc binding moiety. Crystal structures of inhibitors bound to TACE revealed monodentate coordination of the hydantoin to the zinc. SAR, X-ray, and modeling designs are described. To our knowledge, these are the first reported X-ray structures of TACE with a hydantoin zinc ligand. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20172725     DOI： 10.1016/j.bmcl.2010.01.148

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


  9 in total

Review 1.  Targeting Metalloenzymes for Therapeutic Intervention.

Authors:  Allie Y Chen; Rebecca N Adamek; Benjamin L Dick; Cy V Credille; Christine N Morrison; Seth M Cohen
Journal:  Chem Rev       Date:  2018-09-07       Impact factor: 60.622

2.  A novel inhibitor of ADAM17 sensitizes colorectal cancer cells to 5-Fluorouracil by reversing Notch and epithelial-mesenchymal transition in vitro and in vivo.

Authors:  Dan-Dan Li; Chang-Hao Zhao; Huai-Wei Ding; Qiong Wu; Tian-Shu Ren; Jian Wang; Cong-Qin Chen; Qing-Chun Zhao
Journal:  Cell Prolif       Date:  2018-08-02       Impact factor: 6.831

3.  Photochemical Preparation of 1,2-Dihydro-3 H-indazol-3-ones in Aqueous Solvent at Room Temperature.

Authors:  Jie S Zhu; Niklas Kraemer; Clarabella J Li; Makhluf J Haddadin; Mark J Kurth
Journal:  J Org Chem       Date:  2018-12-06       Impact factor: 4.354

4.  Antitumor evaluation and 3D-QSAR studies of a new series of the spiropyrroloquinoline isoindolinone/aza-isoindolinone derivatives by comparative molecular field analysis (CoMFA).

Authors:  Masoud Sadeghzadeh; Maryam Salahinejad; Nahid Zarezadeh; Mehdi Ghandi; Maryam Keshavarz Baghery
Journal:  Mol Divers       Date:  2017-08-23       Impact factor: 2.943

5.  Electrochemical synthesis of N,N'-disubstituted indazolin-3-ones via an intramolecular anodic dehydrogenative N-N coupling reaction.

Authors:  Jessica C Bieniek; Michele Grünewald; Johannes Winter; Dieter Schollmeyer; Siegfried R Waldvogel
Journal:  Chem Sci       Date:  2022-06-13       Impact factor: 9.969

6.  Rapid and halide compatible synthesis of 2-N-substituted indazolone derivatives via photochemical cyclization in aqueous media.

Authors:  Hui-Jun Nie; An-Di Guo; Hai-Xia Lin; Xiao-Hua Chen
Journal:  RSC Adv       Date:  2019-04-30       Impact factor: 4.036

7.  In Silico and Experimental ADAM17 Kinetic Modeling as Basis for Future Screening System for Modulators.

Authors:  Marian Bienstein; Dmitriy Minond; Ulrich Schwaneberg; Mehdi D Davari; Daniela Yildiz
Journal:  Int J Mol Sci       Date:  2022-01-25       Impact factor: 5.923

8.  Synthesis of Succinimide-Linked Indazol-3-ols Derived from Maleimides under Rh(III) Catalysis.

Authors:  Ju Young Kang; Suho Kim; Junghyea Moon; Eunjae Chung; Jaeyoung Kim; So Young Kyung; Hyung Sik Kim; Neeraj Kumar Mishra; In Su Kim
Journal:  ACS Omega       Date:  2022-04-21

9.  Development of Novel 1,3-Disubstituted-2-Thiohydantoin Analogues with Potent Anti-Inflammatory Activity; In Vitro and In Silico Assessments.

Authors:  Salma M Khirallah; Heba M M Ramadan; Ahmed Shawky; Safa H Qahl; Roua S Baty; Nada Alqadri; Amnah Mohammed Alsuhaibani; Mariusz Jaremko; Abdul-Hamid Emwas; Essa M Saied
Journal:  Molecules       Date:  2022-09-23       Impact factor: 4.927
  9 in total

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