Synthesis of Quinoline Motif and Their Virtual HIV Protease Inhibition Analysis, Anti‐Proliferative Probing on HCT116 Cell Line. Issue 25 (4th July 2019)

• Record Type: Journal Article
• Authors: Gopi, P.; Lokesh, R.; Sarveswari, S.
• Is Part Of: ChemistrySelect. Volume 4:Issue 25(2019)
• Page Start: 7627
• Page End: 7633
• Publication Date: 2019-07-04
• Subjects: Cytotoxicity -- Docking -- HCT116 cells -- HIV protease-1 -- Non-peptidic quinoline analogues; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/slct.201901231
• Languages: English
• ISSNs: 2365-6549

Abstract

Abstract: Two diverged series of water‐soluble non‐peptidic quinoline analogues were designed and synthesized by sequential attachment of piperazine and various amino acids to quinoline scaffold at first and second position using peptide coupling procedures. All synthesized compounds were subjected to the in‐silico screening against HIV protease‐1 and the cytotoxicity property of all synthesized compounds was examined on HCT116 cells. The compound, which has threonine and piperazine in sequence at quinoline second position found to have significant HIV protease inhibition property and demonstrated cytotoxicity IC50 value at 22.7±0.59 nM. Abstract : This work aims to invent a multi targeted molecule towards pharmaceutical applications, various diverged quinoline molecules have been designed by using skeletons of few HIV protease inhibitors and synthesised with natural amino acids. All molecules were screened with cytotoxicity study on HCT116 cells and molecular docking with HIV protease‐1. After careful inspection of results of those two experiments, a molecule has been found that was profoundly performed against HIV protease and colorectal cancer cells.