205-30-1Relevant articles and documents
Synthesis and evaluation of the tetracyclic ring-system of isocryptolepine and regioiso-mers for antimalarial, antiproliferative and antimicrobial activities
Albrigtsen, Marte,Andersen, Jeanette H.,Avery, Vicky M.,H?heim, Katja S.,Helgeland, Ida T. Urdal,Kennedy, Emily K.,Lauga, Clémence,Lindb?ck, Emil,Matringe, Théodora,Sydnes, Magne O.,Tan, Kah Ni
, (2021/06/16)
A series of novel quinoline-based tetracyclic ring-systems were synthesized and evaluated in vitro for their antiplasmodial, antiproliferative and antimicrobial activities. The novel hydroiodide salts 10 and 21 showed the most promising antiplasmodial inhibition, with compound 10 displaying higher selectivity than the employed standards. The antiproliferative assay revealed novel pyridophenanthridine 4b to be significantly more active against human prostate cancer (IC50 = 24 nM) than Puromycin (IC50 = 270 nM) and Doxorubicin (IC50 = 830 nM), which are used for clinical treatment. Pyridocarbazoles 9 was also moderately effective against all the employed cancer cell lines and moreover showed excellent biofilm inhibition (9a: MBIC = 100 μM; 9b: MBIC = 100 μM).
