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Synthesis and biological activities of hapalosin derivatives with modification at the C12 position
N Kashihara1, S To-e, K Nakamura
1Department of Chemistry, Faculty of Science and Technology, Keio University, Hiyoshi, Yokohama, Japan.
Bioorganic & Medicinal Chemistry Letters
|February 15, 2000
Abstract:
Among the hapalosin derivatives synthesized, the compounds carrying methyl (5a), methylthioethyl (5d) and phenylmethyl (5e) groups at the C12 position possess only the cis-peptide structure, in contrast to the cases of 5b and 5c. In addition to their conformational stability, the biological activities of the compounds were determined in relation of the P-glycoprotein-mediated MDR-reversing activity and induction of apoptosis.