title: Design and Synthesis of Pyrrolo[2,1-a]Isoquinoline-Based Derivatives as New Cytotoxic Agents.
abstract: A new series of anti-cancer agents based on 1,2-diaryl-5,6-dihydropyrrolo[2,1-a]isoquinoline scaffold containing N,N-diethylamino-ethoxy, piperidinyl-ethoxy or morpholinyl-ethoxy group at theparaposition of the C-2 phenyl ring were synthesized and their cytotoxic activities were assessed against several human cancer cell lines including MCF-7 (ER positive breast cancer cell), MDA-MB231 (ER-negative breast cancer cell), T47D (Human ductal breast epithelial tumor cell line), A549 (adenocarcinomic human alveolar basal epithelial cells), and Hela (human cervix adenocarcinoma cells) using MTT assay. Based on results, compounds, 1-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-5,6-dihydro-8,9-dimethoxy-2-phenylpyrrolo[2,1-a]isoquinoline (6a) and 2-(4-(5,6-dihydro-8,9-dimethoxy-2-phenylpyrrolo[2,1-a] isoquinolin-1-yl)phenoxy)-N,N-diethylethanamine (6c) were the most potent cytotoxic compounds and more toxic than the reference compound against T47D cell line, while all the compounds had satisfactory activity against HeLa cell line with mean IC50values ranging from 1.93 to 33.84 µM.
authors.affiliation: Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti Universityof Medical Sciences, Tehran, Iran. ; Torbat Heydarieh University of Medical Sciences, Torbat Heydarieh, Iran.
authors.forename: Samaneh
authors.initials: S
authors.lastname: Kakhki
authors.affiliation: Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran .
authors.forename: Soraya
authors.initials: S
authors.lastname: Shahosseini
authors.affiliation: Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran .
authors.forename: Afshin
authors.initials: A
authors.lastname: Zarghi
keywords: 1; 1-a]isoquinoline; 2-diaryl-5; 6-dihydropyrrolo[2; Cytotoxic activity; Docking study; MTT; Synthesis