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来自加勒比被囊动物的其他抗肿瘤海鞘素:晶体结构及体内活性

Additional antitumor ecteinascidins from a Caribbean tunicate: crystal structures and activities in vivo.

作者信息

Sakai R, Rinehart K L, Guan Y, Wang A H

机构信息

School of Chemical Sciences, University of Illinois, Urbana 61801.

出版信息

Proc Natl Acad Sci U S A. 1992 Dec 1;89(23):11456-60. doi: 10.1073/pnas.89.23.11456.

Abstract

Ecteinascidins (Ets), isolated from the Caribbean tunicate Ecteinascidia turbinata, protect mice in vivo against P388 lymphoma, B16 melanoma, M5076 ovarian sarcoma, Lewis lung carcinoma, and the LX-1 human lung and MX-1 human mammary carcinoma xenografts. Crystal structures of two tris(tetrahydroisoquinoline) Ets were investigated with single crystals of the 21-O-methyl-N12-formyl derivative of Et 729 and the natural N12-oxide of Et 743. Representatives of an additional class of Ets, Et 722 and Et 736, isolated from the same organism, were assigned tetrahydro-beta-carboline-substituted bis(tetrahydroisoquinoline) structures by NMR and fast atom bombardment MS spectra.

摘要

从加勒比被囊动物Ecteinascidia turbinata中分离出的海鞘素(Ets),可在体内保护小鼠免受P388淋巴瘤、B16黑色素瘤、M5076卵巢肉瘤、Lewis肺癌以及LX - 1人肺癌和MX - 1人乳腺癌异种移植瘤的侵害。利用Et 729的21 - O - 甲基 - N12 - 甲酰基衍生物和Et 743的天然N12 - 氧化物的单晶研究了两种三(四氢异喹啉)Ets的晶体结构。从同一生物体中分离出的另一类Ets的代表,即Et 722和Et 736,通过核磁共振(NMR)和快原子轰击质谱(MS)光谱被确定为四氢 - β - 咔啉取代的双(四氢异喹啉)结构。

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