NDLI: Hemiasterlin analogues incorporating an aromatic, and heterocyclic type C-terminus: design, synthesis and biological evaluation

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Hemiasterlin analogues incorporating an aromatic, and heterocyclic type C-terminus: design, synthesis and biological evaluation

Content Provider	PubMed Central
Author	Giordano, Lesma Sacchetti, Alessandro Bai, Rouli Basso, Giuseppe Bortolozzi, Roberta Hamel, Ernest Silvani, Alessandra Nadia, Vaiana Viola, Giampietro
Copyright Year	2014
Abstract	A representative series of structural analogs of the antimitotic tripeptides hemiasterlins have been designed and synthesized, as potential inhibitors of tubulin polymerization. Relying also on a computational approach, we aimed to explore unknown extensive changes at the C-fragment, by incorporating the conformationally required double bond into five- and six-membered rings. Key steps of the synthetic strategy are a dynamic resolution affording the A-fragment in 97 % ee and the preparation of six new cyclic C fragments, all potentially able to interact with tubulin by means of H bonds. Unexpectedly, biological evaluation of these analogs did not provide evidences neither for cytotoxic effect nor for inhibition of tubulin polymerization.
Related Links	http://dx.doi.org/10.1007/s11030-014-9507-9
Ending Page	373
Page Count	17
Starting Page	357
File Format	PDF
ISSN	13811991
e-ISSN	1573501X
Journal	Molecular diversity
Issue Number	2
Volume Number	18
Language	English
Publisher Date	2014-05-01
Access Restriction	Open
Subject Keyword	Physical and Theoretical Chemistry Inorganic Chemistry Organic Chemistry Molecular Biology Drug Discovery Catalysis Information Systems Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Medicine Drug Discovery Molecular Biology Physical and Theoretical Chemistry Information Systems Catalysis Inorganic Chemistry

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