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- Title
Synthesis of Cyclo- β-tripeptides and Their Biological in vitro Evaluation as Antiproliferatives against the Growth of Human Cancer Cell Lines.
- Authors
Gademann, Karl; Seebach, Dieter
- Abstract
A number of cyclo- β-tripeptides and their linear precursors were subjected to primary biological evaluation for cancer-cell growth inhibition (one-dose, three-cell essay), and the five most active ones were then tested in the anti-tumor screen of the National Cancer Institute (Bethesda, USA) with 60 human cancer cell lines. Growth inhibition values GI50 in the one-digit micromolar, and in one case in the nanomolar range were obtained. The effects show selectivities for certain types of cancer cells and for certain cell lines within these types; the screen includes leukemia, non-small-cell lung, colon, and central-nervous-system (CNS) cancer, melanoma, ovarian, renal, prostate, and breast cancer cell lines. The synthesis and full characterization of two new cyclo- β-peptides, ( β3-HSer(OBn))3 ( 11) and ( β3-HMet)3 ( 12) are described. Other cyclo- β-peptides included in this investigation are ( β-Asp(Bn))3 ( 13), ( β-HGlu(Bn))3 ( 14), and ( β-HAla)3 ( 16), compounds which had been previously prepared by us. Strongest activities were measured with the cyclo- β-peptides bearing benzyl-ester or benzyl-ether groups in the side chains. The cytotoxic activity of the compounds included in this investigation is much lower ( LC50>100 μ M) than their antiproliferative activity ( GI50).
- Publication
Helvetica Chimica Acta, 2001, Vol 84, Issue 10, p2924
- ISSN
0018-019X
- Publication type
Article
- DOI
10.1002/1522-2675(20011017)84:10<2924::AID-HLCA2924>3.0.CO;2-E