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含有甲基 1,2,8,8a-四氢环丙[a]氧杂卓[2,3-e]吲哚-4-酮-6-羧酸酯(COI)烷基化亚单位的 duocarmycin SA 类似物的合成与评价。

Synthesis and evaluation of duocarmycin SA analogs incorporating the methyl 1,2,8,8a-tetrahydrocyclopropa[c]oxazolo[2,3-e]indol-4-one-6-carboxylate (COI) alkylation subunit.

机构信息

Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.

出版信息

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1854-7. doi: 10.1016/j.bmcl.2010.01.145. Epub 2010 Feb 2.

DOI:10.1016/j.bmcl.2010.01.145
PMID:20171886
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2965170/
Abstract

The design, synthesis and evaluation of methyl 1,2,8,8a-tetrahydrocyclopropa[c]oxazolo[2,3-e]indol-4-one-6-carboxylate (COI) derivatives are detailed representing analogs of duocarmycin SA containing an oxazole replacement for the fused pyrrole found in the alkylation subunit.

摘要

详细介绍了甲基 1,2,8,8a-四氢环丙[a]恶唑并[2,3-e]吲哚-4-酮-6-羧酸酯(COI)衍生物的设计、合成和评价,这些衍生物是含有取代稠合吡咯的二羧酸 SA 类似物,其中的恶唑环替代了烷基化亚基中的稠合吡咯。

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本文引用的文献

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An alternative and convenient strategy for generation of substantial quantities of singly 5'-32P-end-labeled double-stranded DNA for binding studies: development of a protocol for examination of functional features of (+)-CC-1065 and the duocarmycins that contribute to their sequence-selective DNA alkylation properties.一种用于生成大量单链 5'-32P 末端标记双链 DNA 以进行结合研究的替代且便捷的策略:开发一种用于研究(+)-CC-1065 和双霉素的功能特征的方案,这些功能特征有助于它们的序列选择性 DNA 烷基化特性。
Tetrahedron. 1991;47(14-15):2661-82.
2
Synthesis and Preliminary Evaluation of Duocarmycin Analogues Incorporating the 1,2,11,11a-Tetrahydrocyclopropa[c]naphtho[2,3-e]indol-4-one (CNI) and 1,2,11,11a-Tetrahydrocyclopropa[c]naphtho[1,2-e]indol-4-one (iso-CNI) Alkylation Subunits.含1,2,11,11a-四氢环丙并[c]萘并[2,3-e]吲哚-4-酮(CNI)和1,2,11,11a-四氢环丙并[c]萘并[1,2-e]吲哚-4-酮(异-CNI)烷基化亚基的多卡霉素类似物的合成与初步评价
Tetrahedron. 2009 Aug 15;65(33):6591-6599. doi: 10.1016/j.tet.2009.02.065.
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