Graphical Abstract Preparation of penta-azole containing cyclopeptides: challenges in macrocyclization
نویسندگان
چکیده
Herein is described the synthesis of several analogs of the natural product IB-01211 from concatenated azoles, via a biomimetic pathway based on cyclization-oxidation of serine containing peptides combined with the Hantzsch synthesis. The macrocyclization of rigid peptide compounds 1 and 2 to give IB-01211 and its epimer 12b was explored, and the results are compared here to those previously obtained for the macrocyclization of more flexible structures in the syntheses of YM-216391, telomestatin, and IB-01211. Lastly, the preliminary results of anti-tumor activity screening of the synthesized analogs are discussed. © 2013 Elsevier Science. All rights reserved ——— Corresponding author. Tel.: +34 93 403 7086; fax: +34 93 403 7126; e-mail: [email protected]; [email protected].
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