2007 Feb 1 .
Synthesis of IB-01211, a Cyclic Peptide Containing 2,4-Concatenated Thia- and Oxazoles, via Hantzsch Macrocyclization.
Hernandez D, Vilar G, Riego E, Canedo LM, Cuevas C, Albericio F, Alvarez M.
Barcelona Science Park Josep Samitier 1-5, E-08028 Barcelona, Spain.
An efficient and versatile convergent synthesis of IB-01211 based on a combination of peptide and heterocyclic chemistry is described. The key step in the synthesis is macrocyclization through intramolecular Hantzsch formation of the thiazole ring. Dehydration of a free primary alcohol to furnish the exocyclic methylidene present in the natural product was applied during the macrocyclization.
05 febrero 2007
Aplidin Small cell lung cancer and targeted therapies.
2007 Mar 19
Small cell lung cancer and targeted therapies.
Blackhall FH , Shepherd FA
aChristie Hospital NHS Trust, Manchester, UK bPrincess Margaret Hospital and the University of Toronto, Toronto, Ontario, Canada.
PURPOSE OF REVIEW: Small cell lung cancer is a chemosensitive malignancy, yet long-term survival remains elusive for the majority of patients. Here, we report on progress in evaluating novel targeted therapies for the treatment of this disease. RECENT FINDINGS: Interferons, matrix metalloproteinase inhibitors, thalidomide, bevacizumab, ZD6474, imatinib, gefitinib, oblimersen and aplidine have all entered clinical trial in patients with small cell lung cancer. Immunotherapy approaches targeting cell surface antigens such as CD-56 (BB10901) and GD3 ganglioside are also being evaluated. Interferons, matrix metalloproteinase inhibitors, imatinib and gefitinib have failed to demonstrate efficacy for this disease. Preliminary data for thalidomide are promising and so results from trials of other antiangiogenics such as bevacizumab and ZD6474 are awaited with interest. SUMMARY: Although the promise of targeted therapy has yet to be realized in patients with small cell lung cancer, the number of agents available for evaluation provides new optimism that progress will be made over the next decades.
Small cell lung cancer and targeted therapies.
Blackhall FH , Shepherd FA
aChristie Hospital NHS Trust, Manchester, UK bPrincess Margaret Hospital and the University of Toronto, Toronto, Ontario, Canada.
PURPOSE OF REVIEW: Small cell lung cancer is a chemosensitive malignancy, yet long-term survival remains elusive for the majority of patients. Here, we report on progress in evaluating novel targeted therapies for the treatment of this disease. RECENT FINDINGS: Interferons, matrix metalloproteinase inhibitors, thalidomide, bevacizumab, ZD6474, imatinib, gefitinib, oblimersen and aplidine have all entered clinical trial in patients with small cell lung cancer. Immunotherapy approaches targeting cell surface antigens such as CD-56 (BB10901) and GD3 ganglioside are also being evaluated. Interferons, matrix metalloproteinase inhibitors, imatinib and gefitinib have failed to demonstrate efficacy for this disease. Preliminary data for thalidomide are promising and so results from trials of other antiangiogenics such as bevacizumab and ZD6474 are awaited with interest. SUMMARY: Although the promise of targeted therapy has yet to be realized in patients with small cell lung cancer, the number of agents available for evaluation provides new optimism that progress will be made over the next decades.
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