海洋毒素多穴海绵苷A类似物的合成及生物学评价

Synthesis and biological evaluation of analogs of the marine toxin polycavernoside A.

作者信息

Barriault L, Boulet S L, Fujiwara K, Murai A, Paquette L A, Yotsu-Yamashita M

机构信息

Evans Chemical Laboratories, The Ohio State University, Columbus 43210, USA.

出版信息

Bioorg Med Chem Lett. 1999 Jul 19;9(14):2069-72. doi: 10.1016/s0960-894x(99)00341-8.

DOI:10.1016/s0960-894x(99)00341-8

PMID:10450983

Abstract

Second generation analogs of polycavemoside A (2) possessing a side chain at C-15 different from that of the natural toxin have been synthesized. The in vivo toxicities of these new compounds (expressed as the minimal lethal dose) have been evaluated in mice (ip) and compared to 2, its aglycone (8), and polycavemoside B (9). The bioactivity profile of enynene 5 is particularly notable.

摘要

已合成了多洞穴苷A（2）的第二代类似物，其在C-15位具有与天然毒素不同的侧链。已在小鼠中（腹腔注射）评估了这些新化合物的体内毒性（以最小致死剂量表示），并与2、其苷元（8）和多洞穴苷B（9）进行了比较。烯炔5的生物活性概况尤为显著。