Acridine as an Anti-Tumour Agent: A Critical Review

This review summarized the current breakthroughs in the chemistry of acridines as anti-cancer agents, including new structural and biologically active acridine attributes. Acridine derivatives are a class of compounds that are being extensively researched as potential anti-cancer drugs. Acridines ar...

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Main Authors: Potlapati Varakumar, Kalirajan Rajagopal, Baliwada Aparna, Kannan Raman, Gowramma Byran, Clara Mariana Gonçalves Lima, Salma Rashid, Mohammed H. Nafady, Talha Bin Emran, Sławomir Wybraniec
Format: Article
Language:English
Published: MDPI AG 2022-12-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/28/1/193
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author Potlapati Varakumar
Kalirajan Rajagopal
Baliwada Aparna
Kannan Raman
Gowramma Byran
Clara Mariana Gonçalves Lima
Salma Rashid
Mohammed H. Nafady
Talha Bin Emran
Sławomir Wybraniec
author_facet Potlapati Varakumar
Kalirajan Rajagopal
Baliwada Aparna
Kannan Raman
Gowramma Byran
Clara Mariana Gonçalves Lima
Salma Rashid
Mohammed H. Nafady
Talha Bin Emran
Sławomir Wybraniec
author_sort Potlapati Varakumar
collection DOAJ
description This review summarized the current breakthroughs in the chemistry of acridines as anti-cancer agents, including new structural and biologically active acridine attributes. Acridine derivatives are a class of compounds that are being extensively researched as potential anti-cancer drugs. Acridines are well-known for their high cytotoxic activity; however, their clinical application is restricted or even excluded as a result of side effects. The photocytotoxicity of propyl acridine acts against leukaemia cell lines, with C1748 being a promising anti-tumour drug against UDP-UGT’s. CK0403 is reported in breast cancer treatment and is more potent than CK0402 against estrogen receptor-negative HER2. Acridine platinum (Pt) complexes have shown specificity on the evaluated DNA sequences; 9-anilinoacridine core, which intercalates DNA, and a methyl triazene DNA-methylating moiety were also studied. Acridine thiourea gold and acridinone derivatives act against cell lines such as MDA-MB-231, SK-BR-3, and MCF-7. Benzimidazole acridine compounds demonstrated cytotoxic activity against Dual Topo and PARP-1. Quinacrine, thiazacridine, and azacridine are reported as anti-cancer agents, which have been reported in the previous decade and were addressed in this review article.
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spelling doaj.art-6878b1de2c624a45b0847b8c6a6b16dd2023-12-03T14:57:06ZengMDPI AGMolecules1420-30492022-12-0128119310.3390/molecules28010193Acridine as an Anti-Tumour Agent: A Critical ReviewPotlapati Varakumar0Kalirajan Rajagopal1Baliwada Aparna2Kannan Raman3Gowramma Byran4Clara Mariana Gonçalves Lima5Salma Rashid6Mohammed H. Nafady7Talha Bin Emran8Sławomir Wybraniec9Department of Pharmaceutical Chemistry, JSS College of Pharmacy (JSS Academy of Higher Education & Research), Ooty 643001, IndiaDepartment of Pharmaceutical Chemistry, JSS College of Pharmacy (JSS Academy of Higher Education & Research), Ooty 643001, IndiaDepartment of Pharmaceutical Chemistry, JSS College of Pharmacy (JSS Academy of Higher Education & Research), Ooty 643001, IndiaDepartment of Pharmaceutical Chemistry, JSS College of Pharmacy (JSS Academy of Higher Education & Research), Ooty 643001, IndiaDepartment of Pharmaceutical Chemistry, JSS College of Pharmacy (JSS Academy of Higher Education & Research), Ooty 643001, IndiaDepartment of Food Science, Federal University of Lavras, Lavras 37200-900, BrazilDepartment of Pharmacy, Faculty of Allied Health Sciences, Daffodil International University, Dhaka 1207, BangladeshFaculty of Applied Health Science Technology, Misr University for Science and Technology, Giza 12568, EgyptDepartment of Pharmacy, Faculty of Allied Health Sciences, Daffodil International University, Dhaka 1207, BangladeshDepartment of Chemical Technology and Environmental Analysis, Faculty of Chemical Engineering and Technology, Cracow University of Technology, Warszawska 24, 31-155 Krakow, PolandThis review summarized the current breakthroughs in the chemistry of acridines as anti-cancer agents, including new structural and biologically active acridine attributes. Acridine derivatives are a class of compounds that are being extensively researched as potential anti-cancer drugs. Acridines are well-known for their high cytotoxic activity; however, their clinical application is restricted or even excluded as a result of side effects. The photocytotoxicity of propyl acridine acts against leukaemia cell lines, with C1748 being a promising anti-tumour drug against UDP-UGT’s. CK0403 is reported in breast cancer treatment and is more potent than CK0402 against estrogen receptor-negative HER2. Acridine platinum (Pt) complexes have shown specificity on the evaluated DNA sequences; 9-anilinoacridine core, which intercalates DNA, and a methyl triazene DNA-methylating moiety were also studied. Acridine thiourea gold and acridinone derivatives act against cell lines such as MDA-MB-231, SK-BR-3, and MCF-7. Benzimidazole acridine compounds demonstrated cytotoxic activity against Dual Topo and PARP-1. Quinacrine, thiazacridine, and azacridine are reported as anti-cancer agents, which have been reported in the previous decade and were addressed in this review article.https://www.mdpi.com/1420-3049/28/1/193acridineanti-cancercancer cell linesDNA-intercalationtopoisomerasein vitro assay
spellingShingle Potlapati Varakumar
Kalirajan Rajagopal
Baliwada Aparna
Kannan Raman
Gowramma Byran
Clara Mariana Gonçalves Lima
Salma Rashid
Mohammed H. Nafady
Talha Bin Emran
Sławomir Wybraniec
Acridine as an Anti-Tumour Agent: A Critical Review
Molecules
acridine
anti-cancer
cancer cell lines
DNA-intercalation
topoisomerase
in vitro assay
title Acridine as an Anti-Tumour Agent: A Critical Review
title_full Acridine as an Anti-Tumour Agent: A Critical Review
title_fullStr Acridine as an Anti-Tumour Agent: A Critical Review
title_full_unstemmed Acridine as an Anti-Tumour Agent: A Critical Review
title_short Acridine as an Anti-Tumour Agent: A Critical Review
title_sort acridine as an anti tumour agent a critical review
topic acridine
anti-cancer
cancer cell lines
DNA-intercalation
topoisomerase
in vitro assay
url https://www.mdpi.com/1420-3049/28/1/193
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AT gowrammabyran acridineasanantitumouragentacriticalreview
AT claramarianagoncalveslima acridineasanantitumouragentacriticalreview
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