RESUMEN
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).
Asunto(s)
Alcaloides Indólicos/farmacología , Quinolinas/síntesis química , Quinolinas/farmacología , Antiinfecciosos/farmacología , Antimaláricos/farmacología , Antineoplásicos/farmacología , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Humanos , Alcaloides Indólicos/metabolismo , Plasmodium falciparum/efectos de los fármacos , Quinolinas/metabolismo , Relación Estructura-ActividadRESUMEN
Eichhornia crassipes is well known as an invasive aquatic plant. It is also used very effectively in phytoremediation, particularly for the rhizofiltration of effluents contaminated by heavy metals. In this article, we show that it is also an excellent bioindicator of water polluted by worrying organic pollutants such as endocrine disruptors and neonicotinoids. As a proof of concept, di-n-hexylphthalate, pentabromodiphenyl ether, nitenpyram, acetamiprid and bis (3-tert-butyl-4-hydroxy-6-methylphenyl) sulfide were clearly identified by UHPLC-HRMS or GC-MS in the root system of E. crassipes after a short period of exposure. These results open up new perspectives for the remediation of water polluted by alarming organic pollutants.