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Title: One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: A unique, highly active antimicrotubule agent
Authors: Romagnoli, Romeo ×
Baraldi, Pier Giovanni
Lopez Cara, Carlota
Kimatrai Salvador, Maria
Bortolozzi, Roberta
Basso, Giuseppe
Viola, Giampietro
Balzarini, Jan
Brancale, Andrea
Fu, Xian-Hua
Zhang, Su-Zhan
Hamel, Ernest #
Issue Date: Dec-2011
Series Title: European Journal of Medicinal Chemistry vol:46 issue:12 pages:6015-6024
Abstract: A wide variety of small molecules with diverse molecular scaffolds inhibit microtubule formation. In this article we report a one-pot procedure for the preparation of a novel 2-(N-pyrrolidinyl)-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole in which the size of the substituent at the C-2 position of the thiazole ring plays an essential role in compound activity. The most active agent (3f) inhibited at submicromolar concentrations the growth of tumor cell lines. It also inhibited tubulin polymerization with an activity quantitatively similar to that of CA-4, and treatment of HeLa cells resulted in their arrest at the G2-M phase of the cell cycle. Furthermore, 3f was effective against multidrug resistant cancer cells and inhibited the growth of the HT-29 xenograft in a nude mouse model. This indicated that 3f is a promising new antimitotic agent with encouraging preclinical potential.
URI: 
ISSN: 0223-5234
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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