TY - JOUR
T1 - Synthesis, solution structure, and bioactivity of six new simplified analogues of the natural cyclodepsipeptide jaspamide
AU - Terracciano, Stefania
AU - Bruno, Ines
AU - Bifulco, Giuseppe
AU - Avallone, Elvira
AU - Smith, Charles D.
AU - Gomez-Paloma, Luigi
AU - Riccio, Raffaele
N1 - Funding Information:
The University of Salerno and the Ministry of Instruction, University and Research (MIUR, Rome), are gratefully acknowledged for financial support of this project through the funds ex-60% and PRIN 2001, 2003 programs, respectively. The use of instrumental facilities of the Competence Center for Diagnostics and Molecular Pharmaceutics, sponsored by Regione Campania POR funds, is gratefully acknowledged. Finally, we thank Prof. Caterina Turco and Ms. Rita Di Giacomo (University of Salerno) for performing apoptosis assays on Jurkat cells.
PY - 2005/9/1
Y1 - 2005/9/1
N2 - Recently, we described the synthesis and the biological evaluation of three modified analogues of jaspamide (1), a natural cyclodepsipeptide possessing a potent antitumor activity as a consequence of its ability to interfere with actin cytoskeleton. To obtain additional information on the potential pharmacophoric core of the target molecule, which is of fundamental importance to discover new and more effective anticancer products, we decided to explore the biological effects of further structural modifications carried out on the parent molecule. The synthesis and the chemical characterization of six jaspamide analogues (2-7) are reported and their conformational and biological properties are described.
AB - Recently, we described the synthesis and the biological evaluation of three modified analogues of jaspamide (1), a natural cyclodepsipeptide possessing a potent antitumor activity as a consequence of its ability to interfere with actin cytoskeleton. To obtain additional information on the potential pharmacophoric core of the target molecule, which is of fundamental importance to discover new and more effective anticancer products, we decided to explore the biological effects of further structural modifications carried out on the parent molecule. The synthesis and the chemical characterization of six jaspamide analogues (2-7) are reported and their conformational and biological properties are described.
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U2 - 10.1016/j.bmc.2005.05.042
DO - 10.1016/j.bmc.2005.05.042
M3 - Article
C2 - 16023351
AN - SCOPUS:22844445699
SN - 0968-0896
VL - 13
SP - 5225
EP - 5239
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 17
ER -