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SAR study of 4,8-disubstituted Pyrimido[5,4-d]pyrimidines exhibiting antitrypan...

Lopes, André; Teixeira, Sofia; Santarém, Nuno; Greco, Alessandro; Pagliaro, Angela; Keminer, Oliver; Gul, Sheraz; Cordeiro-Da-Silva, Anabela

A set of new derivatives of 4,8-disubstituted pyrimido[5,4-d]pyrimidines were efficiently synthesized and in vitro evaluated against Trypanosoma brucei and Leishmania infantum promastigotes and intramacrophage amastigotes. The in vitro cytotoxicity was determined using the THP-1 cell line, and early in vitro ADME-Tox was carried out using in vitro assays for cytotoxicity (A549 and HEK293 cell lines) and CYP3A4 ...


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