Molecular modeling, synthesis, and biological evaluation of macrocyclic calpain inhibitors

Angewandte Chemie
Andrew D AbellRoy Bickerstaffe

Abstract

The design and elaboration of a series of macrocyclic templates that exhibit a propensity to adopt a beta-strand-like peptide-backbone conformation led to potent and selective inhibitors of calpain 2. Macrocycle 1 retarded calcium-induced opacification in an ovine-lens culture assay and is a lead compound for the development of a drug for cataract treatment. Cbz=carbobenzyloxy.

References

Jun 20, 1998·Journal of Medicinal Chemistry·R J CherneyC P Decicco
Mar 15, 2002·Cell·Tudor MoldoveanuPeter L Davies
May 16, 2002·Journal of the American Chemical Society·Robert C ReidDavid P Fairlie
Oct 3, 2003·Biochemical and Biophysical Research Communications·Zhen-Dan ShiTerrence R Burke
Jan 22, 2004·Chemistry : a European Journal·Andreas KrebsMichael W Göbel
Mar 10, 2005·Chemical Reviews·Joel D A TyndallDavid P Fairlie
Nov 24, 2005·Investigative Ophthalmology & Visual Science·Lucinda J G RobertsonMitsuyoshi Azuma
Jan 31, 2006·Angewandte Chemie·Susan E Gibson, Cristina Lecci
Apr 14, 2006·Current Topics in Medicinal Chemistry·Radim VicikTanja Schirmeister
Jul 2, 2008·Nature Reviews. Drug Discovery·Edward M DriggersNicholas K Terrett
Mar 13, 2009·Clinical & Experimental Ophthalmology·Hannah Y Y LeeJames M Coxon

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Citations

Sep 25, 2012·Journal of the American Chemical Society·Hyunil JoDoron C Greenbaum
Oct 1, 2011·Journal of Medicinal Chemistry·Blair G StuartRoy Bickerstaffe
Jan 27, 2012·Journal of Medicinal Chemistry·Sebastian M Saupe, Torsten Steinmetzer
Feb 22, 2012·Organic Letters·Ashok D Pehere, Andrew D Abell
Nov 18, 2015·ACS Chemical Biology·Scott E AllenAlbert A Bowers
Jan 16, 2010·Medicinal Research Reviews·María Jesús Pérez de VegaRosario González-Muñiz
Aug 14, 2015·Journal of Chemical Information and Modeling·Arumugam Ramachandran MuralidharanPitchairaj Geraldine
Oct 6, 2012·The Biochemical Journal·Robert L Campbell, Peter L Davies
Mar 26, 2011·Expert Opinion on Therapeutic Patents·Isaac O Donkor
May 6, 2016·Journal of Medicinal Chemistry·Kristin E LowSerge Zaretsky
Nov 12, 2016·Nature Reviews. Drug Discovery·Yasuko OnoHiroyuki Sorimachi
Nov 18, 2014·Expert Opinion on Therapeutic Patents·Isaac O Donkor
Apr 21, 2012·Chemistry : a European Journal·Victoria PeddieAndrew D Abell
Oct 8, 2014·Angewandte Chemie·Timothy A HillDavid P Fairlie
Sep 30, 2010·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Øyvind JacobsenPål Rongved
Feb 6, 2020·Expert Opinion on Drug Discovery·Levente Endre DókusZoltán Bánóczi
Jul 24, 2020·Chembiochem : a European Journal of Chemical Biology·Aimee J HorsfallAndrew D Abell
Oct 10, 2012·Organic & Biomolecular Chemistry·Ashok D PehereAndrew D Abell
Nov 20, 2012·Chemistry & Biodiversity·Hongyuan ChenAndrew D Abell
Jun 7, 2014·Angewandte Chemie·Krystle C H ChuaAndrew D Abell
Nov 10, 2009·Angewandte Chemie·Noriko OkamotoReiko Yanada
Apr 23, 2013·Chemistry : a European Journal·Ashok D PehereAndrew D Abell
Aug 24, 2020·Bioorganic & Medicinal Chemistry·Fumiya TanakaYuichi Masuda
Apr 29, 2009·The Journal of Organic Chemistry·Andrew D AbellAndrew Muscroft-Taylor
Jul 16, 2021·RSC Medicinal Chemistry·Quynh Ngoc VuYu Heng Lau
Dec 21, 2016·ACS Medicinal Chemistry Letters·Xiaozhou ZhangAndrew D Abell

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