design, synthesis and cytotoxicity evaluation of new 2-aryl-5,6-dihydropyrrolo[2, 1-a]isoquinoline derivatives as topoisomerase inhibitors

Authors

afshin zarghi department of medicinal chemistry, school of pharmacy, shahid beheshti university of medical sciences, tehran, iran

samaneh kakhki department of medicinal chemistry, school of pharmacy, shahid beheshti university of medical sciences, tehran/iran

sorayya shahhoseini department of medicinal chemistry, school of pharmacy, shahid beheshti university of medical sciences, tehran/iran

abstract

two set of 2-aryl-5,6-dihydropyrrolo[2,1-a] isoquinolines were designed and synthesized to evaluate their biological activities as topoisomerase inhibitors. cytotoxic activity of the synthesized compounds 4a-e and 7a-d was assessed against several human cancer cell lines, including mcf-7 (breast cancer cell), hepg2 (liver hepatocellular cells), a549 (adenocarcinomic human alveolar basal epithelial cells), t47d (human ductal breast epithelial tumor cell line) and hela (human cervix cancer). according to our results, hepg2 seems to be the most sensitive cell line for these compounds with mean ic50 values ranging from 4.25 to 70.05 µm. our results indicated that compound 7b exhibited the best potency against the tested cell lines. these results also suggest that pyrroloisoquinoline moiety constitutes a suitable scaffold to design new anti-proliferative agents.

Upgrade to premium to download articles

Sign up to access the full text

Already have an account?login

similar resources

Design, Synthesis and Cytotoxicity Evaluation of New 2-Aryl-5,6-Dihydropyrrolo[2, 1-a]Isoquinoline Derivatives as Topoisomerase Inhibitors

Two set of 2-aryl-5,6-dihydropyrrolo[2,1-a] isoquinolines were designed and synthesized to evaluate their biological activities as topoisomerase inhibitors. Cytotoxic activity of the synthesized compounds 4a-e and 7a-d was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HepG2 (liver hepatocellular cells), A549 (adenocarcinomic human alveolar basal epithel...

full text

Design, Synthesis and Cytotoxicity Evaluation of New 2-Aryl-5,6-Dihydropyrrolo[2, 1-a]Isoquinoline Derivatives as Topoisomerase Inhibitors

Two set of 2-aryl-5,6-dihydropyrrolo[2,1-a] isoquinolines were designed and synthesized to evaluate their biological activities as topoisomerase inhibitors. Cytotoxic activity of the synthesized compounds 4a-e and 7a-d was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HepG2 (liver hepatocellular cells), A549 (adenocarcinomic human alveolar basal epithel...

full text

Design, Synthesis and Cytotoxicity Evaluation of New 2-Aryl-5, 6-Dihydropyrrolo[2, 1-a]Isoquinoline Derivatives as Topoisomerase Inhibitors

Two set of 2-aryl-5, 6-dihydropyrrolo [2,1-a] isoquinolines were designed and synthesized to evaluate their biological activities as topoisomerase inhibitors. Cytotoxic activity of the synthesized compounds 4a-e and 7a-d was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HepG2 (liver hepatocellular cells), A549 (adenocarcinomic human alveolar basal epith...

full text

Design, Synthesis and Evaluation of Substituted Aryl-2-Nitrovinyl Derivatives as Small Molecules Proteasome Inhibitors

Based on the existing structure activity relationship for proteasome inhibitors, a number of substituted aryl-2-nitrovinyl derivatives have been synthesized as Michael acceptor and their cytotoxicity and proteasome inhibitory effects were evaluated on two cancer cell lines. Compound 2d exhibited IC50 values of 0.71 and 17.79 μM comparable to bortezomib against MCF-7 and PC-3, respectively. The ...

full text

Design, Synthesis and Evaluation of Substituted Aryl-2-Nitrovinyl Derivatives as Small Molecules Proteasome Inhibitors

Based on the existing structure activity relationship for proteasome inhibitors, a number of substituted aryl-2-nitrovinyl derivatives have been synthesized as Michael acceptor and their cytotoxicity and proteasome inhibitory effects were evaluated on two cancer cell lines. Compound 2d exhibited IC50 values of 0.71 and 17.79 μM comparable to bortezomib against MCF-7 and PC-3, respectively. The ...

full text

Design, Synthesis and Biological Evaluation of new 1,4-Dihydropyridine (DHP) Derivatives as Selective Cyclooxygenase-2 Inhibitors

As a continuous research for discovery of new COX-2 inhibitors, chemical synthesis, in vitro biological activity and molecular docking study of anew group of 1,4-dihydropyridine (DHP) derivatives were presented. Novel synthesized compounds possessing a COX-2 SO2Me pharmacophore at the para position of C-4 phenyl ring, different hydrophobic groups (R1) at C-2 position and alkoxycarbonyl groups (...

full text

My Resources

Save resource for easier access later


Journal title:
iranian journal of pharmaceutical research

جلد ۱۳، شماره Supplement، صفحات ۷۱-۷۷

Keywords
[ ' k e y w o r d s ' , ' p y r r o l o [ 2 ' , 1 , ' a ] i s o q u i n o l i n e s ' , ' t o p o i s o m e r a s e i n h i b i t o r s ' , ' m o l e c u l a r m o d e l i n g ' , ' c y t o t o x i c i t y ' ]

Hosted on Doprax cloud platform doprax.com

copyright © 2015-2023