187101-52-6Relevant articles and documents
New 2,9-disubstituted-1,10-phenanthroline derivatives with anticancer activity by selective targeting of telomeric G-quadruplex DNA
Craciun, Anda-Mihaela,Rotaru, Alexandru,Cojocaru, Corneliu,Mangalagiu, Ionel I.,Danac, Ramona
, (2021)
Fifteen new 1,10-phenanthrolines disubstituted at positions 2 and 9 via amide bonds with different heterocycles have been designed and synthesized as G-quadruplex DNA stabilizers. Ten compounds were evaluated for the in vitro anticancer activity against 60 human tumor cell lines panel, four of them showing a very good inhibitory activity on several cell lines. To assess the ability of the most active compounds to interact with G-quadruplex DNA (G4-DNA), circular dichroism experiments were performed. The potency of the compounds to stabilize the G4-DNA has been shown from the thermal denaturation experiments. The mechanism of compounds binding to DNA and to G4-DNA was theoretically investigated by molecular docking studies. The experimental results demonstrated excellent capacity of the two compounds bearing two pyridin-3-yl residues (methylated and non-methylated) to act as selective G-quadruplex binders with promising anticancer activity.
2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion
Sayer, James R.,Walldn, Karin,Pesnot, Thomas,Campbell, Frederick,Gane, Paul J.,Simone, Michela,Koss, Hans,Buelens, Floris,Boyle, Timothy P.,Selwood, David L.,Waksman, Gabriel,Tabor, Alethea B.
, p. 6459 - 6470 (2015/01/09)
A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyrazines has been used to probe the structure-activity relationships of these inhibitors, which show potential as antibacterial agents.
SUBSTITUTED 8 - AMINO - IMIDAZO [1, 2-A] PYRAZ1NES AS ANTIBACTERIAL AGENTS
-
, (2013/02/27)
The present invention relates to substituted imidazo[1,2-a]pyrazines of Formula (I) and their use as antibacterial agents.