Synthesis and Evaluation of the Tetracyclic Ring-System of Isocryptolepine and Regioisomers for Antimalarial, Antiproliferative and Antimicrobial Activities

Autor:	Katja S. Håheim, Emil Lindbäck, Kah Ni Tan, Marte Albrigtsen, Ida T. Urdal Helgeland, Clémence Lauga, Théodora Matringe, Emily K. Kennedy, Jeanette H. Andersen, Vicky M. Avery, Magne O. Sydnes
Jazyk:	angličtina
Rok vydání:	2021
Předmět:	indoloquinoline antiplasmodial activity antiproliferative activity antimicrobial activity biofilm inhibition Organic chemistry QD241-441
Zdroj:	Molecules, Vol 26, Iss 11, p 3268 (2021)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules26113268
Popis:	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).
Databáze:	Directory of Open Access Journals
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