Kashihara N, To-e S, Nakamura K, Umezawa K, Yamamura S, Nishiyama S
Department of Chemistry, Faculty of Science and Technology, Keio University, Hiyoshi, Yokohama, Japan.
Bioorg Med Chem Lett. 2000 Jan 17;10(2):101-3. doi: 10.1016/s0960-894x(99)00647-2.
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.
在合成的哈帕洛辛衍生物中，与5b和5c的情况相反，在C12位带有甲基（5a）、甲硫基乙基（5d）和苯甲基（5e）基团的化合物仅具有顺式肽结构。除了其构象稳定性外，还测定了这些化合物与P-糖蛋白介导的多药耐药逆转活性和细胞凋亡诱导相关的生物学活性。
