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Keywords = thiazacridine

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42 pages, 34933 KB  
Review
Acridine as an Anti-Tumour Agent: A Critical Review
by Potlapati Varakumar, Kalirajan Rajagopal, Baliwada Aparna, Kannan Raman, Gowramma Byran, Clara Mariana Gonçalves Lima, Salma Rashid, Mohammed H. Nafady, Talha Bin Emran and Sławomir Wybraniec
Molecules 2023, 28(1), 193; https://doi.org/10.3390/molecules28010193 - 26 Dec 2022
Cited by 57 | Viewed by 8939
Abstract
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 [...] Read more.
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. Full article
(This article belongs to the Special Issue Design, Synthesis and Evaluation of Novel Anticancer Agents)
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16 pages, 693 KB  
Article
Synthesis, DNA Binding and Topoisomerase I Inhibition Activity of Thiazacridine and Imidazacridine Derivatives
by Elizabeth Almeida Lafayette, Sinara Mônica Vitalino de Almeida, Marina Galdino Da Rocha Pitta, Eduardo Isidoro Carneiro Beltrão, Teresinha Gonçalves da Silva, Ricardo Olímpio de Moura, Ivan Da Rocha Pitta, Luiz Bezerra De Carvalho and Maria Do Carmo Alves de Lima
Molecules 2013, 18(12), 15035-15050; https://doi.org/10.3390/molecules181215035 - 6 Dec 2013
Cited by 55 | Viewed by 7872
Abstract
Thiazacridine and imidazacridine derivatives have shown promising results as tumors suppressors in some cancer cell lines. For a better understanding of the mechanism of action of these compounds, binding studies of 5-acridin-9-ylmethylidene-3-amino-2-thioxo-thiazolidin-4-one, 5-acridin-9-ylmethylidene-2-thioxo-thiazolidin-4-one, 5-acridin-9-ylmethylidene-2-thioxo-imidazolidin-4-one and 3-acridin-9-ylmethyl-thiazolidin-2,4-dione with calf thymus DNA (ctDNA) by electronic [...] Read more.
Thiazacridine and imidazacridine derivatives have shown promising results as tumors suppressors in some cancer cell lines. For a better understanding of the mechanism of action of these compounds, binding studies of 5-acridin-9-ylmethylidene-3-amino-2-thioxo-thiazolidin-4-one, 5-acridin-9-ylmethylidene-2-thioxo-thiazolidin-4-one, 5-acridin-9-ylmethylidene-2-thioxo-imidazolidin-4-one and 3-acridin-9-ylmethyl-thiazolidin-2,4-dione with calf thymus DNA (ctDNA) by electronic absorption and fluorescence spectroscopy and circular dichroism spectroscopy were performed. The binding constants ranged from 1.46 × 104 to 6.01 × 104 M−1. UV-Vis, fluorescence and circular dichroism measurements indicated that the compounds interact effectively with ctDNA, both by intercalation or external binding. They demonstrated inhibitory activities to human topoisomerase I, except for 5-acridin-9-ylmethylidene-2-thioxo-1,3-thiazolidin-4-one. These results provide insight into the DNA binding mechanism of imidazacridines and thiazacridines. Full article
(This article belongs to the Section Medicinal Chemistry)
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