Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids

Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids

A small library of cage-like heterocyclic hybrids encompassing pyrroloisoquinolines, pyridinone and acenaphthene structural moieties have been synthesized and tested for their potential as anticancer agents against HCT116 and JURKAT cell lines. The results revealed that these cell lines are more sen...

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Main Authors: Raju Suresh Kumar, Abdulrahman I. Almansour, Natarajan Arumugam, D. Kotresha, Janardhana Papayya Balakrishna
Format: Article
Language:English
Published: Elsevier 2020-12-01
Series:Saudi Journal of Biological Sciences
Subjects:
Cage-like heterocyclic hybrids
HCT116
JURKAT
Apoptosis
Cell cycle
TUNEL Assay
Online Access:http://www.sciencedirect.com/science/article/pii/S1319562X20304484
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spelling doaj-9332b148874345388e6010cf5e0afecc2020-12-03T04:30:33ZengElsevierSaudi Journal of Biological Sciences1319-562X2020-12-01271232903300Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybridsRaju Suresh Kumar0Abdulrahman I. Almansour1Natarajan Arumugam2D. Kotresha3Janardhana Papayya Balakrishna4Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia; Corresponding author.Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi ArabiaDepartment of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi ArabiaDepartment of Botany, Davangere University, Shivagangothri, Davangere- 577007, Karnataka, IndiaDepartment of Stem Cell Biology, Stellixir Biotech Pvt Ltd, No.V-31, 2nd Floor, 10th Main Road, Peenya 2nd Stage Industrial Area, Bangalore 560058, Karnataka, IndiaA small library of cage-like heterocyclic hybrids encompassing pyrroloisoquinolines, pyridinone and acenaphthene structural moieties have been synthesized and tested for their potential as anticancer agents against HCT116 and JURKAT cell lines. The results revealed that these cell lines are more sensitive towards compound 1g and it showed dose dependent cytotoxic effect at 48 hrs of incubation. The IC50 values of compound 1g against HCT116 and JURKAT cell lines are 12.14 ± 1.53 and 10.68 ± 0.68 µM, respectively. Further studies on the determination of mechanism of action of compound 1g discovered that it brought the cell death by inducing Caspase 3 dependent apoptosis and also by arresting the cell cycle at S phase. These studies revealed that compound 1g can be recommended as a potential anti-cancer agent.http://www.sciencedirect.com/science/article/pii/S1319562X20304484Cage-like heterocyclic hybridsHCT116JURKATApoptosisCell cycleTUNEL Assay
collection DOAJ
language English
format Article
sources DOAJ
author Raju Suresh Kumar
Abdulrahman I. Almansour
Natarajan Arumugam
D. Kotresha
Janardhana Papayya Balakrishna
spellingShingle Raju Suresh Kumar
Abdulrahman I. Almansour
Natarajan Arumugam
D. Kotresha
Janardhana Papayya Balakrishna
Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
Saudi Journal of Biological Sciences
Cage-like heterocyclic hybrids
HCT116
JURKAT
Apoptosis
Cell cycle
TUNEL Assay
author_facet Raju Suresh Kumar
Abdulrahman I. Almansour
Natarajan Arumugam
D. Kotresha
Janardhana Papayya Balakrishna
author_sort Raju Suresh Kumar
title Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title_short Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title_full Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title_fullStr Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title_full_unstemmed Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title_sort caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
publisher Elsevier
series Saudi Journal of Biological Sciences
issn 1319-562X
publishDate 2020-12-01
description A small library of cage-like heterocyclic hybrids encompassing pyrroloisoquinolines, pyridinone and acenaphthene structural moieties have been synthesized and tested for their potential as anticancer agents against HCT116 and JURKAT cell lines. The results revealed that these cell lines are more sensitive towards compound 1g and it showed dose dependent cytotoxic effect at 48 hrs of incubation. The IC50 values of compound 1g against HCT116 and JURKAT cell lines are 12.14 ± 1.53 and 10.68 ± 0.68 µM, respectively. Further studies on the determination of mechanism of action of compound 1g discovered that it brought the cell death by inducing Caspase 3 dependent apoptosis and also by arresting the cell cycle at S phase. These studies revealed that compound 1g can be recommended as a potential anti-cancer agent.
topic Cage-like heterocyclic hybrids
HCT116
JURKAT
Apoptosis
Cell cycle
TUNEL Assay
url http://www.sciencedirect.com/science/article/pii/S1319562X20304484
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AT abdulrahmanialmansour caspasedependentapoptoticactivityofpolycycliccagelikeheterocyclichybrids
AT natarajanarumugam caspasedependentapoptoticactivityofpolycycliccagelikeheterocyclichybrids
AT dkotresha caspasedependentapoptoticactivityofpolycycliccagelikeheterocyclichybrids
AT janardhanapapayyabalakrishna caspasedependentapoptoticactivityofpolycycliccagelikeheterocyclichybrids
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