128454-90-0Relevant articles and documents
QUINAZOLINE DERIVATIVES AND THEIR USE AS DNA METHYLTRANSFERASE INHIBITORS
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Page/Page column 43, (2015/04/15)
The present invention relates to compounds of the following formula (I): and pharmaceutically acceptable salts and solvates thereof, their methods of preparation, their use as a drug, notably in the treatment of cancer, and pharmaceutical compositions containing such compounds.
AMINE COMPOUNDS HAVING ANTI-INFLAMMATORY, ANTIFUNGAL, ANTIPARASITIC AND ANTICANCER ACTIVITY
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Page/Page column 141, (2014/08/19)
Amine compounds having activity against inflammation, fungi, unicellular parasitic microorganisms, and cancer are described. The compounds contain a monocyclic, bicyclic, or tricyclic aromatic ring having one, two, or three ring nitrogen atoms.
N-Cinnamoylated chloroquine analogues as dual-stage antimalarial leads
Pérez, Bianca C.,Teixeira, Cátia,Albuquerque, Ine?s S.,Gut, Jiri,Rosenthal, Philip J.,Gomes, José R. B.,Prude?ncio, Miguel,Gomes, Paula
, p. 556 - 567 (2013/04/23)
The control of malaria is challenged by drug resistance, and new antimalarial drugs are needed. New drug discovery efforts include consideration of hybrid compounds as potential multitarget antimalarials. Previous work from our group has demonstrated that hybrid structures resulting from cinnamic acid conjugation with heterocyclic moieties from well-known antimalarials present improved antimalarial activity. Now, we report the synthesis and SAR analysis of an expanded series of cinnamic acid derivatives displaying remarkably high activities against both blood-and liver-stage malaria parasites. Two compounds judged most promising, based on their in vitro activity and druglikeness according to the Lipinski rules and Veber filter, were active in vivo against blood-stage rodent malaria parasites. Therefore, the compounds reported represent a new entry as promising dual-stage antimalarial leads.
Recycling antimalarial leads for cancer: Antiproliferative properties of N-cinnamoyl chloroquine analogues
Perez, Bianca C.,Fernandes, Iva,Mateus, Nuno,Teixeira, Catia,Gomes, Paula
supporting information, p. 6769 - 6772 (2014/01/06)
Cinnamic acids and quinolines are known as useful scaffolds in the discovery of antitumor agents. Therefore, N-cinnamoylated analogues of chloroquine, recently reported as potent dual-action antimalarials, were evaluated against three different cancer cel