Selective Antiproliferative and Apoptotic Effects of 2,6-Diketopiperazines on MDA-MB-231 Triple-Negative Breast Cancer.

ABSTRACT: Diketopiperazines (DKPs) have emerged as promising candidates for treating diverse diseases, particularly cancer. In this context, 2,5-diketopiperazines have been extensively investigated in comparison with 2,6-diketopiperazines. This work explores the selectivity and impact of 2,6-diketopiperazine enantiomers derived from α-amino acids on MDA-MB-231 triple-negative breast cancer cells (TNBC). This subtype of cancer is recognized for its aggressiveness and the lack of effective therapeutic options. The evaluation utilized MTT and flow cytometry assays to examine the impact of 2,6-DPKs on the MDA-MB-231 breast cancer cell line. The obtained IC₅₀ values for compounds 1 and (S)-enantiomers ranged from 4.6 μM to 4.944 mM, where 1 and (S)-2a exhibited the lowest values. The IC₅₀

SUBMITTER: Garrido Gonzalez FP 

PROVIDER: S-EPMC11965977 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature