Synthesis and biological activities of hapalosin derivatives with modification at the C12 position |
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| Authors: | Kashihara N To-e S Nakamura K Umezawa K Yamamura S Nishiyama S |
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| Affiliation: | Department of Chemistry, Faculty of Science and Technology, Keio University, Hiyoshi, Yokohama, Japan. |
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| 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. |
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