Preliminary investigation on biological possessions of Saquinavir‐modified quinoline‐derived azadipeptidomimetics. Issue 2 (17th January 2023)

• Record Type: Journal Article
• Authors: Perumal, Gopi; Govindan, Karthick; Jayaram, Alageswaran; Sundaramoorthi, Sarvesweri; Lin, Wei‐Yu
• Is Part Of: Journal of the Chinese Chemical Society. Volume 70:Issue 2(2023)
• Page Start: 145
• Page End: 158
• Publication Date: 2023-01-17
• Subjects: Azapeptidomimetics -- BSA -- cytotoxicity -- DNA -- HIV‐protease‐1 -- in‐silico; Chemistry -- Periodicals; Electronic journals; 540.5
• DOI: 10.1002/jccs.202200504
• Languages: English
• ISSNs: 0009-4536

Abstract

Abstract: Herein, azadipeptidomimetic molecules were designed and synthesized using a quinoline‐histidine‐amino acid sequence with terminal amino acid modification. In‐silico studies were carried out to evaluate the compound's HIV protease‐1 inhibition temperament. In‐vitro anti‐proliferative possessions of the test compounds were studied by executing a series of experiments, namely DNA binding, bovine serum albumin (BSA) binding capability, and cytotoxicity assay on MCF‐7 cells. The molecule 5j exhibited remarkable results in all experiments; it has an excellent DNA binding constant (3.76 × 10 5 ), higher serum albumin unbound concentration of 5.96%, and a significant antiproliferative effect on MCF‐7 cells with IC50 value 0.31 nM. Abstract : Azadipeptidomimetic molecules were designed and synthesized using a quinoline‐histidine‐amino acid sequence with terminal amino acid modification. 5j exhibited remarkable results in all experiments; it has an excellent DNA binding constant (3.76 × 105), higher serum albumin unbound concentration of 5.96%, and a significant antiproliferative effect on MCF‐7 cells.