46995-89-5Relevant articles and documents
Design, synthesis, antitrypanosomal activity, DNA/RNA binding and in vitro ADME profiling of novel imidazoline-substituted 2-arylbenzimidazoles
Kelly, John M.,Taylor, Martin C.,Baji?, Miroslav,Bokuli?, Ana,Jeli?, Dubravko,Ko?trun, Sanja,Krstulovi?, Luka,Popov, Andrea Bistrovi?,Rai?-Mali?, Silvana,Stojkovi?, Marijana Radi?,Zonji?, Iva
, (2020/09/21)
Novel imidazoline benzimidazole derivatives containing diversely substituted phenoxy moieties were synthesized with the aim of evaluating their antitrypanosomal activity, DNA/RNA binding affinity and in vitro ADME properties. The presence of the diethylaminoethyl subunit in 18a–18c led to enhanced antitrypanosomal potency, particularly for 18a and 18c, which contain unsubstituted and methoxy-substituted phenoxy moieties. They were found to be > 2-fold more potent against African trypanosomes than nifurtimox. Fluorescence and CD spectroscopy, thermal denaturation assays and computational analysis indicated a preference of 18a–18c toward AT-rich DNA and their minor groove binding mode. Replacement of the amidine group with less basic and ionisable nitrogen-containing moieties failed to improve membrane permeability of the investigated compounds. Due to structural diversification, the compounds displayed a range of physico-chemical features resulting in variable in vitro ADME properties, leaving space for further optimization of the biological profiles.
Silver(i) complexes of 3-methoxy-4-hydroxybenzaldehyde thiosemicarbazones and triphenylphosphine: structural, cytotoxicity, and apoptotic studies
Silva, Débora E. S.,Becceneri, Amanda B.,Santiago, Jo?o V. B.,Gomes Neto, José A.,Ellena, Javier,Cominetti, Márcia R.,Pereira, José C. M.,Hannon, Michael J.,Netto, Adelino V. G.
, p. 16474 - 16487 (2020/12/03)
Novel silver(i) complexes of the type [AgCl(PPh3)2(L)] {PPh3 = triphenylphosphine; L = VTSC = 3-methoxy-4-hydroxybenzaldehyde thiosemicarbazone (1); VMTSC = 3-methoxy-4-[2-(morpholine-1-yl)ethoxy]benzaldehyde thiosemicarbazone (2); VPTSC = 3-methoxy-4-[2-
Chalcone and flavone derivatives adopted as aurora kinase inhibitor
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Paragraph 0079; 0080; 0092; 0093, (2017/08/02)
The present invention relates to design and synthesis of a class of chalcone and flavone derivatives represented by formulas I (I-1 and I-2) and II (II-1 and II-2), and inhibition effects of the derivatives on aurora kinase A. According to the present inv