757951-78-3Relevant academic research and scientific papers
SYNTHESIS OF DUOCARMYCIN ANALOGUES
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, (2016/12/22)
A novel Fmoc protected duocarmycin subunit of formula (I) and utilisation as a reagent in solid phase protein synthesis methodology. Also provided is a novel method of solid phase peptide synthesis, and in particular a method for the production of novel i
Synthesis and evaluation of duocarmycin SA analogs incorporating the methyl 1,2,8,8a-tetrahydrocyclopropa[c]imidazolo[4,5-e]indol-4-one-6-carboxylate (CImI) alkylation subunit
Chanda, Prem B.,Boyle, Kristopher E.,Brody, Daniel M.,Shukla, Vyom,Boger, Dale L.
, p. 4779 - 4786 (2016/10/05)
The design, synthesis, and evaluation of methyl 1,2,8,8a-tetrahydrocyclopropa[c]imidazolo[4,5-e]indol-4-one-6-carboxylate (CImI) derivatives are detailed representing analogs of duocarmycin SA and yatakemycin containing an imidazole replacement for the fused pyrrole found in the DNA alkylation subunit.
Solid-Phase Synthesis of Duocarmycin Analogues and the Effect of C-Terminal Substitution on Biological Activity
Stephenson, Michael J.,Howell, Lesley A.,O'Connell, Maria A.,Fox, Keith R.,Adcock, Claire,Kingston, Jenny,Sheldrake, Helen,Pors, Klaus,Collingwood, Stephen P.,Searcey, Mark
, p. 9454 - 9457 (2015/10/12)
The duocarmycins are potent antitumor agents with potential for use in the development of antibody-drug conjugates (ADCs) as well as being clinical candidates in their own right. In this article, we describe the synthesis of a duocarmycin monomer (DSA) th
New synthetic method for indole-2-carboxylate and its application to the total synthesis of duocarmycin SA
Hiroya, Kou,Matsumoto, Shigemitsu,Sakamoto, Takao
, p. 2953 - 2956 (2007/10/03)
(Equation Presented) The sequential coupling and cyclization reactions between aryl halides and methyl propiolate were investigated. The electron-withdrawing groups on the aromatic ring are essential for producing the methyl indole-2-carboxylate derivativ
