International Journal of Basic and Applied Medical Sciences ISSN: 2277-2103 (Online) An Online International Journal Available at http://www.cibtech.org/jms.htm 2011 Vol. 1 (1) September-December, pp.18-22/Selvi et al. Research Article 18 SYNTHESIS AND IN-VITRO EVALUATION OF COPOLYESTER- CHALCONE DERIVATIVES AS POTENTIAL ANTICANCER AGENTS *R. Senthamizh Selvi 1 , R. Nanthini 2 and G. Sukanyaa 3 1-2 Postgraduate and Research Department of Chemistry, Pachaiyappa’s College, Chennai-600 030 3 Queen Mary’s College for Women (Autonomous), Chennai-600 005 *Author for Correspondence ABSTRACT A new series of copolyester chalcone derivatives were synthesised from 1, 3-bis (4-hydroxy-3- methoxyphenyl) propenone (BHMPP) and 1- (3, 5-dihydroxyphenyl)-3-(4-methoxyphenyl) propenone (DHPMPP) with adipoyl, suberoyl, azeloyl and sebacoyl chlorides by phase transfer catalysed polycondensation method. The microstructure of the repeating unit was confirmed by IR, 1 H and 13 C NMR. These copolyesters are evaluated for anticancer activity. These chalcone derivatives showed good activity against HepG2 cells with IC 50 values. Key Words: Chalcones, Copolyesters, Polycondensation, Anticancer Agents INTRODUCTION The family of polyesters comprises all polymers with ester functional groups in the polymer back bone. In principle, the synthesis of polyesters or esters in the presence of large amount of water has only been studied by a few research groups. (Saam et al., 1982) studied the polycondensation in suspension of hydrophobic diol and diacid compounds using different sulfonate surfactants (Edlund et al., 2003; Carothers et al., 1929). Copolyesters, obtained from a multiplicity of reactions having the component groups linked in a random or statistical order, are termed random copolyesters. They retain their strength, clarity and other mechanical properties, despite being exposed to a variety of chemicals that typically affect other materials, such as polycarbonates. This includes their versatility and flexibility which enhances their application effectively in the design of high-volume, low cast parts as well as critical, more expensive component parts. Phase transfer catalysis is a synthetic technique which involves transport of an organic or inorganic salt form a solid or aqueous phase into an organic/liquid phase where reaction with an organic soluble substrate takes place. Chalcones are 1, 3-diphenyl-2-propene-1-one, in which two aromatic rings are linked by a three carbon α, β-unsaturated carbonyl system. They possess conjugated double bonds and a completely delocalised π- electron system on both benzene rings. Molecules possessing such system have relatively low redox potentials and have a greater probability of undergoing electron transfer reactions. They represent an essential group of natural as well as synthetic products and some of them possess wide range of pharmacological activity such as antibacterial (Ahmed Kamel et al., 2010) antitumour (Siva Kumar et al., 2007) anticancer (Francesco et al., 2007) anti-inflammatory (Won et al., 2005) antioxidant (Calliste et al., 2001) antimalarial (Liu et al., 2001) antiulcerative (Mukarami et al., 1991) antitubercular (Rajendra Prasad et al., 2008) etc. The presence of reactive α, β-unsaturated keto group in chalcones is found to be responsible for their biological activity (Nowakowska et al., 2008). Chalcones are natural or synthetic flavonoids displaying an impressive array of biological properties. Chalcone constitute an important group of natural products and some of them possess a wide range of biological activities such as anticancer and (Jevwon et al., 2005), antitubercular (Shiva kumar et al., 2007). The anticancer activity of certain chalcones is believed to be a result of binding to tubulin and preventing it from polymerizing into microtubules. Tubulin exists as a heterodimer of two homologous α- and β- subunits. This dimer can couple together to make profilaments consisting of alternating α- and β-subunits. Compounds such as these that target tumour vasculature clearly have significant clinical promise for the