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The paper presents a simple synthesis of new quinazolinone derivatives 13a-i. Synthesized derivatives were tested for their cytotoxic effect against three cancer cell lines including SKLU-1, MCF-7 and HepG-2. The bioassay result showed that only compound 13e exhibited significant cytotoxic effect against cancer cell lines tested with IC50 values of 9.48, 20.39 and 18.04 µg/ mL, respectively.


6-Hydroxy-4(3H) quinazolinone, cytotoxic, cancer

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Ferlay J, Colombet M and Soerjomataram I. Global and Regional Estimates of the Incidence and Mortality for 38 Cancers: GLOBOCAN 2018. Lyon: International Agency for Research on Cancer/World Health Organization; 2018.

Mellinghoff, I. K.; Sawyers, C. L. The emergence of resistance to targeted cancer therapeutics. Pharmacogenomics., 3 (2002), 603- 623.

Welsch ME, Snyder SA, Stockwell BR. Privileged scaffolds for library design and drug discovery. Curr Opin Chem Biol., 14, (2010)1–15.

Asif M.Various chemical and biological activities of pyridazinone derivatives. Cent Eur J Exp Biol., 5 (2017), 1–19.

Nikaljea AP, Bahetia K. Computer based drug design of various heterocyclic compounds having anticancer activity: a brief review. J Bioinform Genom Proteom., (2),1–13 (2017).

Yadav, M. R.; Naik, P. P.; Gandhi, H. P.; Chauhan, B. S.; Giridhar. Design and synthesis of 6,7-dimethoxyquinazoline analogs as multi-targeted ligands for α1- and AII-receptors antagonism. Bioorg. Med. Chem. Lett., 23 (2013), 3959–3966.

Venkatesh, R.; Ramaiah, M. J.; Gaikwad, H. K.; Janardhan, S.; Bantu, R.; Nagarapu, L.; Sastry, G. N.; Ganesh, A. R.; Bhadra, M. Luotonin-A based quinazolinones cause apoptosis and senescence via HDAC inhibition and activation of tumor suppressor proteins in HeLa cells. Eur. J. Med. Chem., 87 (2015), 94-101.

Kamal, A.; Tamboli, J. R.; Ramaiah, M. J.; Adil, S. F.; Pushpavalli, V. L..; Ganesh, R.; Sarma, R.; Bhadra, U.; Bhadra, M. P. Quinazolino linked 4β-amidopodophyllotoxin conjugates regulate angiogenic pathway and control breast cancer cell proliferation. Bioorg. Med. Chem., 21 (2013), 21, 6414–6426.

(a). Shetha, A. & Wijdan, I.A. Synthesis and characterization of new quinazoline–4(3H)-one Schiff bases. J Chem Pharm Res., 5 (2013) 42–45; (b). Amer M. Alanazi, Alaa A.-M. Abdel-Aziz, Ibrahim A. Al-Suwaidan, Sami G. Abdel-Hamide, Taghreed Z. Shawer, Adel S. El-Azab. Design, synthesis and biological evaluation of some novel substituted quinazolines as antitumor agents. Eur. J. Med. Chem., 79 (2014), 446-454 (c) Malleshappa N. Noolvi Harun M. Patel. Synthesis, method optimization, anticancer activity of 2,3,7-trisubstituted Quinazoline derivatives and targeting EGFR-tyrosine kinase by rational approach: 1st Cancer Update. Arab.J.Chem., 6 (2013),35-48; (d). D. H. Fleita, R. M. Mohareb, O. K. Sakka. Antitumor and antileishmanial evaluation of novel heterocycles derived from quinazoline scaffold: a molecular modeling approach. Med. Chem. Res., 22 (2013), 2207-2221.

Zaranappa et al. Synthesis and Antioxidant Activity of 3-Substituted Schiff bases of Quinazoline-2,4-diones. Int J Chem Tech Res., 4 (2012), 1527–1533.

Krishnan, S.K. et al. Synthesis, antiviral and cytotoxic investigation of 2-phenyl-3-substituted quinazolin-4(3H)-ones. Eur Rev Med Pharm Sci., 15 (2011), 673–681.

Patel, N.B. et al. Synthesis and microbial studies of (4-oxo-thiazolidinyl) sulfonamides bearing quinazolin-4(3H) ones. Acta Polo Pharm Drug Res., 67 (2010), 267–275.

Saravanan, G., Pannerselvam, P. & Prakash, C.R. Synthesis, analgesic and anti-inflammatory screening of novel Schiff bases of 3-amino-2-methyl quinazolin 4-(3H)-one. Der Pharmacia Lett., 2 (2010), 216–226.

Abid, O.H. & Ahmed, A.H. Synthesis and characterization of novel quinazoline derivatives via reaction of isatoic anhydride with schiff’s base. Inter J Appl Nat Sci., 2 (2013), 11–20.

Pati, B. & Banerjee, S. Quinazolines: an illustrated review. J Adv Pharm Edu Res., 3 (2013), 136–151.

Katrin, S.N. Chemotherapy and Dietary Phytochemical Agents. Chem ther Res Prac., 3 (2012), 22–27.

Manasa, A.K., Sidhaye, R.V., Radhika, G. & Nalini, C.N. Synthesis, antioxidant and anticancer activity of quinazoline derivatives. Current Pharma Research., 1 (2011), 101–105.

Nerkar, B., Saxena, A., Ghone, S. & Thakeri, A.K. In Silico Screening, Synthesis and In Vitro Evaluation of Some Quinazolinone and Pyridine Derivatives as Dihydrofolate Reductase Inhibitors for Anticancer Activity. E-Journal of Chem., 6 (2009), 97–102.

Danilov, A.V. Targeted therapy in chronic lymphocytic leukemia: past, present, and future. Clin Ther., 35 (2013), 1258–1270.

Ahmed, M. F. & Youns, M. Synthesis and Biological Evaluation of a Novel Series of 6, 8‐Dibromo‐4 (3H) quinazolinone Derivatives as Anticancer Agents. Archiv der Pharmazie., 346 (2013), 610–617.

Kumar, D. Design, synthesis and cytotoxic evaluation of novel imidazolone fused quinazolinone derivatives. Arabian J. Chem. doi: 10.1016/j.arabjc.2014.07.001 (2014).

Faraj, F.L. et al. Synthesis, Characterization, and Anticancer Activity of New Quinazoline Derivatives against MCF-7 Cells. Sci. Wld J. 212096; doi: 10.1155/2014/212096 (2014).

Scudiero, D. A.; Shoemaker, R.H.; Paull, K.D.; Monks, A.; Tierney, S.; Nofziger, T.H.; Currens, M. J.; Seniff, D.; Boyd, M. Feasibility of drug screening with panels of human tumor cell lines using a microculture tetrazolium assay. Cancer Res., 48 (1988), 4827–4833.

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