Articolul precedent |
Articolul urmator |
598 19 |
Ultima descărcare din IBN: 2024-02-22 08:19 |
Căutarea după subiecte similare conform CZU |
547.7/.8:615.011 (2) |
Chimie organică (475) |
Farmacologie. Terapeutică. Toxicologie (1572) |
SM ISO690:2012 AMĂRANDI, Roxana Maria, AL-MATARNEH, Maria-Cristina, POPOVICI, Lacramioara, MANGALAGIU, Ionel I., BEJAN, Vasilichia, CIOBANU, Catalina Ionica, DANAC, Ramona. Pyrrolo-fused heterocyclic derivatives: design, synthesis and anticancer evaluation. In: New frontiers in natural product chemistry.: A destiny on the altar of research. Dedicated to academician Pavel Vlad, Ed. 6, 21 mai 2021, Chișinău. Chișinău, Republica Moldova: Tipografia "Artpoligraf", 2021, Ediția 6, p. 24. ISBN 978-9975-3336-7-2. DOI: https://doi.org/10.19261/nfnpc.2021.ab17 |
EXPORT metadate: Google Scholar Crossref CERIF DataCite Dublin Core |
New frontiers in natural product chemistry. Ediția 6, 2021 |
|
Conferința " New frontiers in natural product chemistry." 6, Chișinău, Moldova, 21 mai 2021 | |
|
|
DOI: https://doi.org/10.19261/nfnpc.2021.ab17 | |
CZU: 547.7/.8:615.011 | |
Pag. 24-24 | |
Descarcă PDF | |
Rezumat | |
Natural compounds with quinoline and isoquinoline scaffolds have demonstrated numerous biological activities and have found use in both medical research laboratories and clinical practice throughout the world [1]. In particular, semisynthetic pyrroloquinoline derivatives are currently widely accepted as first line treatments for anticancer therapy, including camptothecin derivatives irinotecan and topotecan, with many others currently being investigated as potent antiproliferative agents [2]. In addition to pyrrolo(iso)quinolines, which unsurprisingly lie at the center of various synthetic organic chemisty efforts for further improvement of biological activity, including our own group’s [3], other heterocyles can be considered for pyrrole fusion in order to maximize selectivity to targets and improve biological effects, including benzo[f]quinoline, pyrazine and pyrimidine [4]. We describe herein the design, synthesis and anticancer evaluation of novel pyrrolo-fused heterocycles based on quinoline, isoquinoline, benzo[f]quinoline, pyrazine and pyrimidine. We furthermore show that the most active compound from the whole series (pyrrolo[1,2-a]quinoline 10a) inhibits tubulin polymerization in vitro and we describe the in silico molecular interactions with tubulin in order to understand the mechanisms behind its antiproliferative activity. |
|
|