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

نویسندگان

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

چکیده

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.

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

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...

متن کامل

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...

متن کامل

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...

متن کامل

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 ...

متن کامل

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 ...

متن کامل

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 (...

متن کامل

منابع من

با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید


عنوان ژورنال:
iranian journal of pharmaceutical research

جلد ۱۳، شماره Supplement، صفحات ۷۱-۷۷

کلمات کلیدی
[ ' 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 ' ]

میزبانی شده توسط پلتفرم ابری doprax.com

copyright © 2015-2023