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1,8-Naphthalimide derivatives: new leads against dynamin I GTPase activity.
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2015 (English)In: Organic and biomolecular chemistry, ISSN 1477-0520, E-ISSN 1477-0539, Vol. 13, no 29Article in journal (Refereed) Published
Abstract [en]

Fragment-based in silico screening against dynamin I (dynI) GTPase activity identified the 1,8-naphthalimide framework as a potential scaffold for the design of new inhibitors targeting the GTP binding pocket of dynI. Structure-based design, synthesis and subsequent optimization resulted in the development of a library of 1,8-naphthalimide derivatives, called the Naphthaladyn™ series, with compounds 23 and 29 being the most active (IC50 of 19.1 ± 0.3 and 18.5 ± 1.7 μM respectively). Compound 29 showed effective inhibition of clathrin-mediated endocytosis (IC50(CME) 66 μM). The results introduce 29 as an optimised GTP-competitive lead Naphthaladyn™ compound for the further development of naphthalimide-based dynI GTPase inhibitors.

Place, publisher, year, edition, pages
2015. Vol. 13, no 29
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Organic Chemistry
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URN: urn:nbn:se:uu:diva-272663DOI: 10.1039/c5ob00751hPubMedID: 26118967OAI: oai:DiVA.org:uu-272663DiVA: diva2:894545
Available from: 2016-01-15 Created: 2016-01-15 Last updated: 2017-11-30

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Odell, Luke R

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