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Molecules 2010, 15(6), 4085-4093; doi:10.3390/molecules15064085
Article

Synthesis and Biological Evaluation of a γ-Cyclodextrin-based Formulation of the Anticancer Agent 5,6,11,12,17,18,23,24- Octahydrocyclododeca[1,2-b:4,5-b’:7,8-b’’:10,11-b’’’]tetraindole (CTet)

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1 Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Urbino “Carlo Bo” I- 61029 Urbino, Piazza del Rinascimento 6, Italy 2 Dipartimento di Scienze Biomolecolari, Università degli Studi di Urbino “Carlo Bo” I-61029 Urbino, Via Aurelio Saffi 2, Italy
* Author to whom correspondence should be addressed.
Received: 21 April 2010 / Revised: 27 May 2010 / Accepted: 1 June 2010 / Published: 4 June 2010
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Abstract

5,6,11,12,17,18,23,24-octahydrocyclododeca[1,2-b:4,5-b’:7,8-b’’:10,11- b’’’]tetrai ndole (CTet), an indole-3-carbinol (I3C) metabolite endowed with anticancer properties, is poorly soluble in the solvents most frequently used in biological tests. This study indicates that the use of γ-cyclodextrin (γ-CD) avoids this problem. Formulated with γ-CD CTet is a potent inhibitor of DNA synthesis in both estrogen receptor positive (MCF-7) and estrogen receptor negative (MDA-MB-231) human breast cell lines (IC50 = 1.20 ± 0.04 μM and 1.0 ± 0.1 μM, respectively).
Keywords: indole-3-carbinol; indole cyclic tetramer; γ-cyclodextrin; breast cancer indole-3-carbinol; indole cyclic tetramer; γ-cyclodextrin; breast cancer
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Lucarini, S.; De Santi, M.; Antonietti, F.; Brandi, G.; Diamantini, G.; Fraternale, A.; Paoletti, M.F.; Tontini, A.; Magnani, M.; Duranti, A. Synthesis and Biological Evaluation of a γ-Cyclodextrin-based Formulation of the Anticancer Agent 5,6,11,12,17,18,23,24- Octahydrocyclododeca[1,2-b:4,5-b’:7,8-b’’:10,11-b’’’]tetraindole (CTet). Molecules 2010, 15, 4085-4093.

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