Details

Autor(en) / Beteiligte

• Žukauskas, Mindaugas
• Grybaitė, Birutė
• Jonutė, Paulina
• Vaickelionienė, Rita
• Gibieža, Paulius
• Vaickelionis, Giedrius
• Dragūnaitė, Bertina
• Anusevičius, Kazimieras
• Mickevičius, Vytautas
• Petrikaitė, Vilma

Titel

Evaluation of N-aryl-β-alanine derivatives as anticancer agents in triple-negative breast cancer and glioblastoma in vitro models

Ist Teil von

• Bioorganic chemistry, 2021-10, Vol.115, p.105214-105214, Article 105214

Ort / Verlag

United States: Elsevier Inc

Erscheinungsjahr

2021

Quelle

Access via ScienceDirect (Elsevier)

Beschreibungen/Notizen

• [Display omitted] •β-amino acids derivatives bearing hydrazone and azole moieties was synthesized.•Promising compounds against cancer cell lines contain 4-BrPh or 4-ClPh moieties.•Two selected drug candidates showed migrastatic effect on MDA-MB-231 cell line. Synthesis of β-amino acid derivatives containing hydrazone and azole moieties is described. For this purpose, the appropriate hydrazide was treated with aromatic aldehydes, ketones and phenyl iso(thio)cyanates to obtain the desired outcome. The synthesized target compounds were evaluated for their anticancer properties. The assay displayed 3,3′-((2,6-diethylphenyl)azanediyl)bis(N′-(benzylidene)propanehydrazide) to possess the convincing anticancer effect against triple-negative breast cancer cells in vitro. To further study the anticancer properties of compounds containing a hydrazone moiety in breast cancer, series of previously and newly prepared dihydrazones were investigated. It was determined that derivatives with the bis(N′-(4-bromobenzylidene) fragment in the structure are exclusively cytotoxic to cancer cells. The most active compounds against both cell lines were those containing electron withdrawing 4-BrPh or 4-ClPh moieties, together with either chlorine, bromine or iodine groups in para position of phenyl ring. Selected two representative compounds showed migrastatic activity in MDA-MB-231 cell line, where both of them reduced the growth of breast cancer and glioblastoma cell 3D cultures and inhibited cell colony formation. 2009 Elsevier Ltd. All rights reserved.