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Synthesis and biological activities of hapalosin derivatives with modification at the C12 position

✍ Scribed by Nobuki Kashihara; Sakino To-e; Kensuke Nakamura; Kazuo Umezawa; Shosuke Yamamura; Shigeru Nishiyama

Publisher: Elsevier Science
Year: 2000
Tongue: English
Weight: 129 KB
Volume: 10
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(99)00647-2

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✦ Synopsis

AbstractÐAmong 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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