1,8-Naphthalimide derivatives: new leads against dynamin I GTPase activity.

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Fältnamn	Indikatorer	Metadata
000		02117naa a2200361 4500
001		oai:DiVA.org:uu-272663
003		SwePub
008		160115s2015 \| \|\|\|\|\|\|\|\|\|\|\|000 \|\|eng\|
024	7	a https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-2726632 URI
024	7	a https://doi.org/10.1039/c5ob00751h2 DOI
040		a (SwePub)uu
041		a engb eng
042		9 SwePub
072	7	a ref2 swepub-contenttype
072	7	a art2 swepub-publicationtype
100	1	a Abdel-Hamid, Mohammed K4 aut
245	1 0	a 1,8-Naphthalimide derivatives :b new leads against dynamin I GTPase activity.
264		c 2015
264	1	b Royal Society of Chemistry (RSC),c 2015
338		a print2 rdacarrier
520		a 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.
650	7	a NATURVETENSKAPx Kemix Organisk kemi0 (SwePub)104052 hsv//swe
650	7	a NATURAL SCIENCESx Chemical Sciencesx Organic Chemistry0 (SwePub)104052 hsv//eng
700	1	a Macgregor, Kylie A4 aut
700	1	a Odell, Luke R4 aut
700	1	a Chau, Ngoc4 aut
700	1	a Mariana, Anna4 aut
700	1	a Whiting, Ainslie4 aut
700	1	a Robinson, Phillip J4 aut
700	1	a McCluskey, Adam4 aut
773	0	t Organic and biomolecular chemistryd : Royal Society of Chemistry (RSC)g 13:29q 13:29x 1477-0520x 1477-0539
856	4 8	u https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-272663
856	4 8	u https://doi.org/10.1039/c5ob00751h

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Av författaren/redakt...: Abdel-Hamid, Moh ...; Macgregor, Kylie ...; Odell, Luke R; Chau, Ngoc; Mariana, Anna; Whiting, Ainslie; visa fler...; Robinson, Philli ...; McCluskey, Adam; visa färre...

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