57508-53-9Relevant academic research and scientific papers
Tetrazine-mediated bioorthogonal prodrug-prodrug activation
Neumann, Kevin,Gambardella, Alessia,Lilienkampf, Annamaria,Bradley, Mark
, p. 7198 - 7203 (2018)
The selective and biocompatible activation of prodrugs within complex biological systems remains a key challenge in medical chemistry and chemical biology. Herein we report, for the first time, a dual prodrug activation strategy that fully satisfies the principle of bioorthogonality by the symbiotic formation of two active drugs. This dual and traceless prodrug activation strategy takes advantage of the INVDA chemistry of tetrazines (here a prodrug), generating a pyridazine-based miR21 inhibitor and the anti-cancer drug camptothecin and offers a new concept in prodrug activation.
Synthesis and structure of aroylamidines and N-arylbenzamidines hydrochlorides
Kuvaeva,Fedorova,Zaitsev,Yakovlev,Zakharov,Semakova
experimental part, p. 209 - 213 (2012/06/01)
Aroylamidines can be obtained as salts in a reaction of the corresponding arylcarbonitriles with anhydrous ethanol in the presence of dry HCl followed by treating intermediate imidoesters with alcoholic solution of ammonia. N-Arylbenzamidines are obtained by reacting benzonitrile with arylamines in the presence of AlCl3. The structure of arylamines and the reaction conditions signifi cantly affect the yield of the target product, and sometimes the very possibility of its preparation. Pleiades Publishing, Ltd., 2012.
DNA Binding Compounds. VI. Synthesis and Characterization of 2,5'-Disubstituted Bibenzimidazoles Related to the DNA Minor Groove Hoechst 33258
Kelly, David P.,Bateman, Stuart A.,Hook, Robert J.,Martin, Roger F.,Reum, Monica E.,et al.
, p. 1751 - 1770 (2007/10/02)
A series of compounds have been synthesized in which the basic 2-phenylbibenzimidazole structure of Hoechst 33258 has been modified to include various combinations of bromo, iodo, methoxy, amino, alkylamino and nitro groups in the terminal phenyl ring.Both sequential and convergent synthetic routs have been followed using coupling reactions of both imino ethers and aldehydes to 1,2-diamines.All these compounds were characterized by a combination of f.a.b. mass spectrometry and 1H and 13C n.m.r. spectroscopy including inverse detection of long-range heteronuclear CH correlations (HMBC).
