160820-17-7Relevant academic research and scientific papers
Deglycobleomycin A6 analogues modified in the methylvalerate moiety
Cai, Xiaoqing,Zaleski, Paul A.,Cagir, Ali,Hecht, Sidney M.
, p. 3831 - 3844 (2011/08/02)
Previous studies have indicated that the methylvalerate subunit of bleomycin (BLM) plays an important role in facilitating DNA cleavage by BLM and deglycoBLM. Eleven methylvalerate analogues have been synthesized and incorporated into deglycoBLM congeners by the use of solid-phase synthesis. The effect of the valerate moiety in the deglycoBLM analogues has been studied by comparison with the parent deglycoBLM A5 using supercoiled DNA relaxation and sequence-selective DNA cleavage assays. All of the deglycoBLM analogues were found to effect the relaxation of the plasmid DNA. Those analogues having aromatic C4-substituents exhibited cleavage efficiency comparable to that of deglycoBLM A5. Some, but not all, of the deglycoBLM analogues were also capable of mediating sequence-selective DNA cleavage.
Design and synthesis of β-amino-α-hydroxy amide derivatives as inhibitors of MetAP2 and HUVEC growth
Sendzik, Martin,Janc, James W.,Cabuslay, Ronnel,Honigberg, Lee,Mackman, Richard L.,Magill, Catherine,Squires, Neil,Waldeck, Nancy
, p. 3181 - 3184 (2007/10/03)
The rational design and synthesis of β-amino-α-hydroxy amide derivatives as reversible inhibitors of methionine aminopeptidase-2 (MetAP2) with anti-proliferative activity against human umbilical vein endothelial cells (HUVECs) is described.
3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2
Sheppard, George S.,Wang, Jieyi,Kawai, Megumi,BaMaung, Nwe Y.,Craig, Richard A.,Erickson, Scott A.,Lynch, Linda,Patel, Jyoti,Yang, Fan,Searle, Xenia B.,Lou, Pingping,Park, Chang,Kim, Ki H.,Henkin, Jack,Lesniewski, Richard
, p. 865 - 868 (2007/10/03)
Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allow
Hydrazide and alkoxyamide angiogenesis inhibitors
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, (2008/06/13)
Compounds having the formula are methionine aminopeptidase type 2 (MetAP2) inhibitors and are useful for inhibiting angiogenesis. Also disclosed are MetAP2-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.
Alkylation of camphor and pinanone imines of 2-(aminomethyl)thiazole. Enantioselective synthesis of 2-(1-aminoalkyl)thiazoles
Dondoni, Alessandro,Merchan, Francisco L.,Merino, Pedro,Rojo, Isabel,Tejero, Tomas
, p. 641 - 646 (2007/10/03)
A method is described for the enantioselective synthesis of 2-(1-aminoalkyl)thiazoles 6 via stereoselective alkylation of the carbanions of (+)-(R)-camphor and (-)-(1S, 2S, 5S)-2-hydroxypinan-3-one imines 2 and 3 derived from 2-(aminomethyl)thiazole (2-AMT, 1). Compounds 6 serve as α-amino aldehyde precursors via thiazolyl-to-formyl conversion.
