Pyrrolo-fused heterocyclic derivatives: design, synthesis and anticancer evaluation
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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
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New frontiers in natural product chemistry.
Ediția 6, 2021
Conferința " New frontiers in natural product chemistry."
6, Chișinău, Moldova, 21 mai 2021

Pyrrolo-fused heterocyclic derivatives: design, synthesis and anticancer evaluation
DOI:https://doi.org/10.19261/nfnpc.2021.ab17
CZU: 547.7/.8:615.011

Pag. 24-24

Amărandi Roxana Maria12, Al-Matarneh Maria-Cristina13, Popovici Lacramioara1, Mangalagiu Ionel I.1, Bejan Vasilichia1, Ciobanu Catalina Ionica1, Danac Ramona1
 
1 Alexandru Ioan Cuza University of Iaşi,
2 Regional Institute of Oncology Iaşi,
3 “Petru Poni” Institute of Macromolecular Chemistry
 
 
Disponibil în IBN: 28 mai 2021
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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.

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