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Identification of Pyrrolo[3′,4’:3,4]cyclohepta[1,2-d][1,2]oxazoles as Promising New Candidates for the Treatment of Lymphomas by Marilia Barreca; Virginia Spanò; Roberta Rocca; Roberta Bivacqua; Gianmarco Gualtieri; Maria Valeria Raimondi; Eugenio Gaudio; Roberta Bortolozzi; Lorenzo Manfreda; Ruoli Bai; Alessandra Montalbano; Stefano Alcaro; Ernest Hamel; Francesco Bertoni; Giampietro Viola; Paola Barraja is a Chemistry article available to read on EtoBox.

What is Identification of Pyrrolo[3′,4’:3,4]cyclohepta[1,2-d][1,2]oxazoles as Promising New Candidates for the Treatment of Lymphomas about?

Unsatisfactory outcomes for relapsed/refractory lymphoma patients prompt continuing efforts to develop new therapeutic strategies. Our previous studies on pyrrole-based anti-lymphoma agents led us to synthesize a new series of twenty-six pyrrolo[3′,4':3,4]cyclohepta[1,2-d] [1,2]oxazole derivatives and study their antiproliferative effects against a panel of four non-Hodgkin lymphoma cell lines. Several candidates showed significant anti-proliferative effects, with IC50's reaching the sub-micromolar range in at least one cell line, with compound 3z demonstrating sub-micromolar growth inhibitory effects towards the entire panel. The VL51 cell line was the most sensitive, with an IC50 value of 0.10 μM for 3z. Our earlier studies had shown that tubulin was a prominent target of many of our oxazole derivatives. We therefore examined their effects on tubulin assembly and colchicine binding. While 3u and 3z did not appear to target tubulin, good activity was observed with 3d and 3p. Molecular docking and molecular dynamics simulations allowed us to rationalize the binding mode of the synthesized compounds toward tubulin. All ligands exhibited a better affinity for the colchicine site, con

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Author

Marilia Barreca; Virginia Spanò; Roberta Rocca; Roberta Bivacqua; Gianmarco Gualtieri; Maria Valeria Raimondi; Eugenio Gaudio; Roberta Bortolozzi; Lorenzo Manfreda; Ruoli Bai; Alessandra Montalbano; Stefano Alcaro; Ernest Hamel; Francesco Bertoni; Giampietro Viola; Paola Barraja

Publisher

Elsevier BV

Published

2023

Language

EN

Field

Chemistry (Physical Sciences)