Discovery of indolizine lactones as anticancer agents and their optimization through late-stage functionalization

Silva, Thiago Sabino da; Souza, Matheus da Silva; Andricopulo, Adriano D.; Coelho, Fernando

doi:10.1039/d3ra03395c

Cited by 5 publications

(1 citation statement)

References 41 publications

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“…Pyrrole derivatives have exhibited a wide range of pharmacological activities and have been integrated into numerous medications targeting conditions such as inflammation, insomnia, migraines, Parkinson's disease, and erectile dysfunction. 9 Recently, fostemsavir received approval for the treatment of HIV. Pyrrolopyridine scaffolds, such as those found in Vemurafenib and Pexidartinib, show promise as anticancer agents.…”

Section: Introductionmentioning

confidence: 99%

New monoquaternary salts of N-heterocycles: synthesis and antitumor assessment

SARDARU,

AL MATARNEH,

SIMIONESCU

et al. 2024

Rev.Roum.Chim.

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This manuscript presents the synthesis, structural characterization, and antitumor evaluation of new monoquaternary salts derived from various N-heterocycles. For quinoline and quinoxaline, respectively, unexpected H-bonded mixtures of the reactants have been obtained. To assess their potential antitumor activity, the comprehensive panel of NCI's 60 human cancer cell lines was employed. Remarkably, mixtures 3g and 3h displayed significant inhibitory activity against leukemia, melanoma, and colon cancer cell lines. Furthermore, mixtures 3g and 3h displayed good cytotoxicity on MCF7 breast cancer cells, but not on normal fibroblasts, at 2.5x10-5 M, showing promise for therapeutic applications.

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Section: Introductionmentioning

confidence: 99%