Subscribe to our Newsletter and get informed about new publication regulary and special discounts for subscribers!

ILCPA > Volume 73 > Synthesis and Biological Evaluation of Chalcones...
< Back to Volume

Synthesis and Biological Evaluation of Chalcones Possessing Ring Activating Groups as Potent of Anticancer Agents

Full Text PDF


Some novel anticancer agents based on chalcone scaffold were synthesized with potential therapeutic application for many types of cancer. Hydroxy and methoxy substitution on aryl ring of chalcone, depending upon positions in aryl ring influence anticancer and other activities. These chalcone molecules were evaluated for their invitro cytotoxic activity against five cancer cell lines including human chronic myelogenus-leukemia K-562, human breast adenocarcinoma MCF-7, human prostate carcinoma DU-145, human lung adenocarcinoma A-549 and normal VERO cell line. Most of the compounds being active cytotoxic agents and were shown to be non-toxic to normal cells. The synthesized compounds were characterized by means of their FT-IR, MASS and 1HNMR spectral study.


International Letters of Chemistry, Physics and Astronomy (Volume 73)
M. M. Khanusiya and Z. M. Gadhawala, "Synthesis and Biological Evaluation of Chalcones Possessing Ring Activating Groups as Potent of Anticancer Agents", International Letters of Chemistry, Physics and Astronomy, Vol. 73, pp. 1-8, 2017
Online since:
Apr 2017

[1] C.A. Colliste et al., Chalcone structural requirements for antioxidant, estrogenic and antiproliferative activities, Anticancer Res. 21 (2001) 3949-3956.

[2] B. Ngameni, V. Kuete, P. Ambassa, Synthesis and evaluation of anticancer activity of O-allylchalcone derivatives, Medicinal Chemistry. 3 (2013) 233-237.

[3] K. Chandrabose et al., Advances in chalcones with anticancer activities, Recent Patents on Anticancer Drug Discovery. 10(1) (2015) 97-115.

DOI: 10.2174/1574892809666140819153902

[4] S. Lust et al., Xanthohumol kills B-chronic lymphocytic leukemia cells by an apoptotic mechanism, Mol. Nutr. Food Res. 49 (2005) 844-850.

DOI: 10.1002/mnfr.200500045

[5] L. Pan, H. Becker, C. Gerhauser, Xanthohumol induces apoptosis in cultured 40-16 human colon cancer cell by activation of the death receptor and mitochondrial pathway, Molecular Nutrition and Food Research. 49(9) (2005) 873-843.

DOI: 10.1002/mnfr.200500065

[6] C.C. Yit, N.P. Das, Cytotoxic effect of butein on human colon adenocarcinoma cell proliferation, Cancer Lett. 82(1) (1994) 65-72.

DOI: 10.1016/0304-3835(94)90147-3

[7] X. Zi, A.R. Simmoneau, A. Flavokawain, A novel chalcone from kava extract induces apoptosis in bladder cancer cell by involvement of Bax protein dependent and mitochondrial dependent apoptosis and suppresses tumour growth in mice, Cancer Res. 65 (2005).

DOI: 10.1158/0008-5472.can-04-3803

[8] F. Chimenti et al., Chalcones: A valid scaffold for monoamine oxidases inhibitors, J. Med. Chem. 52(9) (2009) 2818-2824.

[9] S. Ducki, Antimitotic chalcones and related compounds as inhibitors of tubulin assembly, Anti-Cancer Agents in Medicinal Chemistry. 9(3) (2009) 336-347.

DOI: 10.2174/1871520610909030336

[10] A. Kamal et al., Synthesis and anticancer activity of chalcone-pyrrolobenzodiazepine conjugates linked via 1, 2, 3-triazole ring side-armed with alkane spacers, European Journal of Medicinal Chemistry. 46(9) (2011) 3820-3831.

DOI: 10.1016/j.ejmech.2011.05.050

[11] T. Narender et al., A new chemical access for 3'-acetyl-4'-hydroxychalcones using borontrifluoride–etherate via a regioselective Claisen-Schmidt condensation and its application in the synthesis of chalcone hybrids, Tetrahedron Lett. 52(44) (2011).

DOI: 10.1016/j.tetlet.2011.08.120

[12] P. Rajakumar, S. Raja, Synthesis, optical and thermal studies of dendritic architectures with chalcone surface groups, Tetrahedron Lett. 49(46) (2008) 6539-6542.

DOI: 10.1016/j.tetlet.2008.09.005

[13] S. Syam et al., Synthesis of chalcones with anticancer activities, Molecules. 17(6) (2012) 6179-6195.

DOI: 10.3390/molecules17066179

[14] R. Pingaew et al., Synthesis, biological evaluation and molecular docking of novel chalcone–coumarin hybrids as anticancer and antimalarial agents, Eur. J. Med. Chem. 85 (2014) 65-76.

DOI: 10.1016/j.ejmech.2014.07.087

[15] M.M. Khanusiya, Z.M. Gadhawala, Synthesis and characterisation of biologically potent novel chalcone moieties, Oriental Journal of Chemistry. 32(2) (2016) 1181-1186.

DOI: 10.13005/ojc/320244

[16] H. Iqbal et al., Synthesis, anti-inflammatory and antioxidant activity of ring-A-monosubstituted chalcone derivatives, Med. Chem. Res. 23(10) (2014) 4383-4394.

DOI: 10.1007/s00044-014-1007-z

[17] G. Thirunarayanan, K. Ravi, Synthesis and spectral correlation study of some 3-(3, 4-dichlorophenyl)-5-(substituted Phenyl)-4, 5-dihydro-1H-Pyrazole-1-yl-Ethanones, International Letters of Chemistry, Physics, and Astronomy. 19 (2013) 44-57.

DOI: 10.18052/

[18] K.G. Sekar, G. Thirunarayanan, Synthesis and spectral studies of some N-[(E)-Phenylmethylidene]benzenesulfonamides, International Letters of Chemistry, Physics, and Astronomy. 13 (2013) 249-258.

DOI: 10.18052/

[19] C.A. Calliste et al., Chalcones: structural requirements for antioxidant, estrogenic and antiproliferative activities, Anticancer Res. 21 (2001) 3949-3956.

[20] S.K. Kumar et al., Design, synthesis, and evaluation of novel boronic-chalcone derivatives as antitumor agents, Journal of Medicinal Chemistry. 46(14) (2003) 2813-2815.

[21] S.P. Bahekar et al., Synthesis of some sulfonamide chalcones of biological interest, International Journal of Chemical and Physical Science. 4 (2015) 99-104.

[22] N.M. Hamada, N.Y.M. Abdo, Synthesis, characterization, antimicrobial screening and free-radical scavenging activity of some novel substituted pyrazoles, Molecules. 20(6) (2015) 10468-10486.

DOI: 10.3390/molecules200610468

[23] A.M. Abdula, Synthesis, characterization and antibacterial activity of (E)-chalcone derivatives, European Journal of Chemistry. 4(3) (2013) 207-210.

[24] R. Arulkumaran et al., Spectral correlations and antimicrobial activities of some 1-pyrenyl chalcones, International Letters of Chemistry, Physics, and Astronomy. 10 (2013) 21-38.

[25] K. Ranganathan et al., Electrochemical reduction potential correlation of some insect antifeedant potent 2-phenothiazinyl chalcones, International Letters of Chemistry, Physics, and Astronomy. 4 (2012) 66-75.

DOI: 10.18052/

[26] S.D. Tala et al., Synthesis and biological study of some new chalcone and pyrazole derivatives, Indian Journal of Chemistry. B. 52 (2013) 807-809.

[27] R.S. Dhivare, S.S. Rajput, Microwave assisted synthesis and antimicrobial screening of novel 9-(N-phenyl) - 4, 5-(2", ‴-methoxyphenol)-9H-1, 3, 6, 8, 9-hexa-azo-fluorene-2, 7-diamine derivatives using bis-heterocyclic chalcones, International Journal of Advances in Pharmacy, Biology and Chemistry. 4(4) (2015).

[28] H. Suwito et al., Chalcones: Synthesis, structure diversity and pharmacological aspects, Journal of Chemical and Pharmaceutical Research. 6(5) (2014) 1076-1088.

Show More Hide