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海兔毒素B的大环酮类似物

Macrocyclic ketone analogues of halichondrin B.

作者信息

Zheng Wanjun, Seletsky Boris M, Palme Monica H, Lydon Paul J, Singer Lori A, Chase Charles E, Lemelin Charles A, Shen Yongchun, Davis Heather, Tremblay Lynda, Towle Murray J, Salvato Kathleen A, Wels Bruce F, Aalfs Kimberley K, Kishi Yoshito, Littlefield Bruce A, Yu Melvin J

机构信息

Department of Medicinal Chemistry, Eisai Research Institute, 4 Corporate Drive, Andover, MA 01810, USA.

出版信息

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5551-4. doi: 10.1016/j.bmcl.2004.08.069.

DOI:10.1016/j.bmcl.2004.08.069

PMID:15482922

Abstract

Structurally simplified macrocyclic ketone analogues of halichondrin B were prepared by total synthesis and found to retain the potent cell growth inhibitory activity in vitro, stability in mouse serum, and in vivo efficacy of the natural product.

摘要

通过全合成制备了结构简化的海兔毒素B大环酮类似物，发现其在体外保留了强大的细胞生长抑制活性、在小鼠血清中的稳定性以及天然产物的体内功效。