Synthesis, Characterisation and Anticancer Study of Acridine derivatives
DOI:
https://doi.org/10.61280/tjpls.v10i5.146Keywords:
Acridine, MTT assay, Anticancer activity, Anticancer drugsAbstract
Cancer is one of the global problem and a major cause for mortality. many treatment strategies are available for cancer treatment, still there is a scope for novel treatment to avoid serious side effects of existing therapy. Novel DNA binding agents are needed for effective treatment of cancers. In the field of antitumor DNA-intercalating agents, 9-aminoacridines play an important role due to their antiproliferative properties. Several cancer chemotherapeutics such as amsacrine and nitracrine have been developed as anticancer agents.In present study, a series of new acridine-based derivatives numbered 3a–3j were synthesized and their anticancer activity against A549 (Human, small cell Lung Carcinoma) cell line was evaluated by MTT Assay. Out of the screened compounds, compound 3b exhibited potent anticancer activity with IC50 78.04 µg/ml for lung cancer cell (A-549) line.Further in vivo study of newly synthesized acridine derivative can explore a ray of light in the field of anticancer drugs.
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References
I. Kumler, N. Brunner, J. Stenvang, E. Balslev, D.L. Nielsen, A systematic review on
Topoisomerase-I inhibition in the treatment of metastatic breast cancer, Breast Cancer Res.
Treat. 138 (2013), 347–358.
X. Zhang, B. Bao, X.H. Yu, et al., The discovery and optimization of novel dual inhibitors
of topoisomerase II and histone deacetylase, Bioorg. Med. Chem. 21 (2013) 6981–6995.
S.M.B. Nijman, S.H. Friend, Cancer. Potential of the synthetic lethality principle, Science
(2013), 809–811.
Y. Li, H.B. Zhang, W.L. Huang, X. Zhen, Y.M. Li, Synthesis and biological evaluation of
tetrahydroisoquinoline derivatives as potential multidrug resistance reversal agents in
cancer,Chin. Chem. Lett. 19 (2008) 169–171.
L.H. Shen, Y. Li, D.H. Zhang, Y.S. Lai, L.J. Liu, Synthesis and evaluation of nitrate
derivatives of colchicine as anticancer agents, Chin. Chem. Lett. 22 (2011) 768– 770.
C. Kaplan-Ozen, B. Tekiner-Gulbas, E. Foto, et al., Benzothiazole derivatives as human
DNAtopoisomerase II alpha inhibitors, Med. Chem. Res. 22 (2013) 5798– 5808.
Z.Y. Tian, H.X. Ma, S.Q. Xie, et al., Synthesis, DNA binding and topoisomerase inhibition
of mononaphthalimide homospermidine derivatives, Chin. Chem. Lett. 19 (2008) 509–512.
J.R. Goodell, A.V. Ougolkov, H. Hiasa, et al., Acridine-based agents with topoisomerase II
activity inhibit pancreatic cancer cell proliferation and induce apoptosis, J. Med. Chem. 51
(2012) 179–182.
K. Padget, A. Stewart, P. Charlton, M.J. Tilby, C.A. Austin, An investigation into the
formation of N-2-(dimethylamino)ethyl acridine-4-carboxamide (DACA) and 6- 2-
(dimethylamino) ethylamino-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one dihydrochloride
(TAS-103) stabilised DNA topoisomerase I and II cleavable complexes in human leukaemia
cells, Biochem. Pharmacol. 60 (2000) 817–821
J.Y. Chang, C.F. Lin, W.Y. Pan, et al., New analogues of AHMA as potential antitumor
agents: synthesis and biological activity, Bioorg. Med. Chem. 11 (2003) 4959–4969
K. Rastogi, J.Y. Chang, W.Y. Pan, et al., Antitumor AHMA linked to DNA minor groove
binding agents: synthesis and biological evaluation, J. Med. Chem. 45 (2002) 4485–4493.
R. Zittoun, m-AMSA: a review of clinical data, Eur. J. Cancer Clin. Oncol. 21 (1985)
–653.
T.L. Su, T.C. Chou, J.Y. Kim, et al., 9-Substituted acridine-derivatives with long half-life
and potent antitumor-activity-synthesis and structure–activity-relationships, J. Med.
Chem. 38 (1995) 3226–3235.
I. Gonzalez-Sanchez, J.D. Solano, M.A. Loza-Mejia, et al., Antineoplastic activity of the
thiazolo 5, 4-b quinoline derivative D3CLP in K-562 cells is mediated through effector
caspases activation, Eur. J. Med. Chem. 46 (2011) 2102–2108.
C.H. Chen, Y.W. Lin, X.G. Zhang, et al., Synthesis and in vitro cytotoxicity of 9-
anilinoacridines bearing N-mustard residue on both anilino and acridine rings, Eur. J.
Med. Chem. 44 (2009) 3056–3059.
X.D. Luan, C.M. Gao, N.N. Zhang, et al., Exploration of acridine scaffold as a potentially
interesting scaffold for discovering novel multi-target VEGFR-2 and Src kinase
inhibitors, Bioorg. Med. Chem.19 (2011) 3312– 3319
Y.Q. Li, C.Y. Tan, C.M. Gao, et al., Discovery of benzimidazole derivatives as novel
multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors, Bioorg. Med. Chem. 19
(2011) 4529–4535.
X.L. Lang, L.L. Li, Y.Z. Chen, et al., Novel synthetic acridine derivatives as potent DNA-
binding and apoptosis-inducing antitumor agents, Bioorg. Med. Chem. 21 (2013) 4170–
X.L. Lang, Q.S. Sun, Y.Z. Chen, et al., Novel synthetic 9-benzyloxyacridine analogue as
both tyrosine kinase and topoisomerase I inhibitor, Chin. Chem. Lett. 24 (2013) 677–680.
C.M. Gao, F. Liu, X.D. Luan, et al., Novel synthetic 2-amino-10-(3, 5-dimethoxy)
benzyl-9(10H)-acridinone derivatives as potent DNA-binding antiproliferative agents,
Bioorg. Med. Chem. 18 (2010) 7507–7514.
C.M. Gao, S.F. Li, X.L. Lang, et al., Synthesis and evaluation of 10-(3, 5-
dimethoxy)benzyl-9(10H)- acridone derivatives as selective telomeric G-quadruplex
DNA ligands, Tetrahedron 68 (2012) 7920–7925.
X.D. Luan, C.M. Gao, Q.S. Sun, et al., Novel synthetic azaacridine analogues as
Topoisomerase-I inhibitors, Chem. Lett. 40 (2011) 728–729.
X.L. Lang, X.D. Luan, C.M. Gao, Y.Y. Jiang, Recent progress of acridine derivatives with
antitumor activity, Prog. Chem. 24 (2012) 1497–1505.
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