Abstract

The triple-negative breast cancer (TNBC) is characterized by a more aggressive nature and poorer prognosis, nowadays none pharmaceutical approach is still available. For this reason, the research of new active compounds and attractive targets represents an interesting field. In this context MDA- MB-231 cell line was selected to evaluate the antiproliferative effects of new [1,2-a]-pyrroloquinoxaline derivatives. The MTT assay revealed that the amine forms of synthesized molecules were more active compared to iminic ones at 72 h of incubation. The antiproliferative effect of the most promising compounds highlighted the formation of autophagic vacuoles.

Highlights

  • Breast cancer (BC) is a heterogeneous and complex disease and one of the leading causes of death in 40–59 years old women

  • To determine whether the new derivatives provide the desired triple-negative breast cancer (TNBC) antiproliferative activity, MDA-MB-231 cell line, were exposed to several concentration of L1-6 L8-10 for 24 or 72 h and cell viability was assessed by MTT assay Figures 1A,B

  • To the best of our knowledge, the in vitro results obtained in this study, it is possible to confirm the versatility of the pyrroloquinoxaline nucleus that once again showed interesting antiproliferative activity assessed with MTT assay

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Summary

Introduction

Breast cancer (BC) is a heterogeneous and complex disease and one of the leading causes of death in 40–59 years old women. TNBC is characterized by low estrogen and progesterone receptors expressions as well as low HER2/Neu amplification. Treatment options beyond the conventional chemotherapy include EGFR, VEGF, and PARP inhibitors (Dawson et al, 2009). These last have shown a strong component of nitrogenous nuclei. Studies performed on TNBC cell line have shown an antiproliferative activity for molecules endowing a pyrroloquinoxaline nucleus, the pyrrolo[2,3-b]quinoxalines. Other studies were performed on breast cancer cell lines expressing the G protein-coupled estrogen receptor (GPER o GPR30) and was evaluated and attributed an antiproliferative activity to molecules with pyrrole[1,2-a]quinoxaline structure (Aiello et al, 2017)

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