Literature DB >> 20399648

Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III.

Yongchun Shen1, Roch Boivin, Naoki Yoneda, Hong Du, Shawn Schiller, Tomohiro Matsushima, Masaki Goto, Hiroshi Shirota, Fabian Gusovsky, Charles Lemelin, Yimin Jiang, Zhiyi Zhang, Robert Pelletier, Megumi Ikemori-Kawada, Yoshiyuki Kawakami, Atsushi Inoue, Matthew Schnaderbeck, Yuan Wang.   

Abstract

Inspired by natural product, LL-Z1640-2, clinical candidate, E6201 (22) was discovered in a medicinal chemistry effort through total synthesis. The modification on C14-position to N-alkyl substitution showed to be potent in vitro and orally active in vivo in anti-inflammatory assays. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20399648     DOI： 10.1016/j.bmcl.2010.03.087

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


  11 in total

1.  Kinase inhibition by deoxy analogues of the resorcylic lactone L-783277.

Authors:  Marc Liniger; Christian Neuhaus; Tatjana Hofmann; Luca Fransioli-Ignazio; Michel Jordi; Peter Drueckes; Jörg Trappe; Doriano Fabbro; Karl-Heinz Altmann
Journal:  ACS Med Chem Lett       Date:  2010-10-20       Impact factor: 4.345

2.  Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.

Authors:  Jin Xu; Anqi Chen; Mei-Lin Go; Kassoum Nacro; Boping Liu; Christina L L Chai
Journal:  ACS Med Chem Lett       Date:  2011-07-17       Impact factor: 4.345

3.  Effects of (5Z)-7-oxozeaenol on MDA-MB-231 breast cancer cells.

Authors:  Ulyana Muñoz Acuña; Jennifer Wittwer; Sloan Ayers; Cedric J Pearce; Nicholas H Oberlies; Esperanza J Carcache DE Blanco
Journal:  Anticancer Res       Date:  2012-07       Impact factor: 2.435

4.  Effects of (5Z)-7-oxozeaenol on the oxidative pathway of cancer cells.

Authors:  Ulyana Muñoz Acuña; Jennifer Wittwer; Sloan Ayers; Cedric J Pearce; Nicholas H Oberlies; Esperanza J Carcache DE Blanco
Journal:  Anticancer Res       Date:  2012-07       Impact factor: 2.435

5.  Use of kinase inhibitors to correct ΔF508-CFTR function.

Authors:  Agata M Trzcinska-Daneluti; Leo Nguyen; Chong Jiang; Christopher Fladd; David Uehling; Michael Prakesch; Rima Al-awar; Daniela Rotin
Journal:  Mol Cell Proteomics       Date:  2012-06-14       Impact factor: 7.381

6.  Novel TRPV1 Modulators with Reduced Pungency Induce Analgesic Effects in Mice.

Authors:  Anny Treat; Vianie Henri; Junke Liu; Joyce Shen; Mauricio Gil-Silva; Alejandro Morales; Avaneesh Rade; Kevin Joseph Tidgewell; Benedict Kolber; Young Shen
Journal:  ACS Omega       Date:  2022-01-10

7.  TGF-β-activated kinase-1 inhibitor LL-Z1640-2 reduces joint inflammation and bone destruction in mouse models of rheumatoid arthritis by inhibiting NLRP3 inflammasome, TACE, TNF-α and RANKL expression.

Authors:  Hirofumi Tenshin; Jumpei Teramachi; Mohannad Ashtar; Masahiro Hiasa; Yusuke Inoue; Asuka Oda; Kotaro Tanimoto; So Shimizu; Yoshiki Higa; Takeshi Harada; Masahiro Oura; Kimiko Sogabe; Tomoyo Hara; Ryohei Sumitani; Tomoko Maruhashi; Mayu Sebe; Rie Tsutsumi; Hiroshi Sakaue; Itsuro Endo; Toshio Matsumoto; Eiji Tanaka; Masahiro Abe
Journal:  Clin Transl Immunology       Date:  2022-01-19

8.  Sensitivity to the MEK inhibitor E6201 in melanoma cells is associated with mutant BRAF and wildtype PTEN status.

Authors:  Sara A Byron; David C Loch; Candice L Wellens; Andreas Wortmann; Jiayi Wu; John Wang; Kenichi Nomoto; Pamela M Pollock
Journal:  Mol Cancer       Date:  2012-10-05       Impact factor: 27.401

9.  TAK1 inhibition-induced RIP1-dependent apoptosis in murine macrophages relies on constitutive TNF-α signaling and ROS production.

Authors:  Jang-Shiun Wang; Dean Wu; Duen-Yi Huang; Wan-Wan Lin
Journal:  J Biomed Sci       Date:  2015-09-18       Impact factor: 8.410

10.  Safety, pharmacokinetics, and preliminary efficacy of E6201 in patients with advanced solid tumours, including melanoma: results of a phase 1 study.

Authors:  Raoul Tibes; Mitesh J Borad; Corina E Dutcus; Larisa Reyderman; Kevie Feit; Andrew Eisen; David A Verbel; Daniel D Von Hoff
Journal:  Br J Cancer       Date:  2018-06-05       Impact factor: 7.640
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