Online ISSN: 2515-8260

DESIGN, SYNTHESIS AND CHARACTERIZATION OF THIAZOLIDINE-2, 4-DIONE ANALOGUES AS ANTI-CANCER AGENTS

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Ganesh Prasad Patel, Akash Yadav, Naveen Gupta, Dharmendra Singh Rajput

Abstract

Compounds with halogen group substitution on aromatic ring exhibited promising activity. Compound 3i with the 2,3-dichloro group at the phenyl ring attached to heterocyclic thiazolidine-2,4-dione showed potent activity against HeLa cells when compared with reference drug adriamycin. Substitution at R with electron withdrawing groups such as chloro, bromo, iodo in compounds 3a, 3b, 3f, 3g and 3i showed increase in activity. The electron donating groups such as methoxy, ethoxy, methyl, ethyl and hydroxy substituted compounds 3c, 3e, 3j, 3l, 3m, 3o, 3p, 3r showed decrease in activity. The compound 3i with 2, 3-dichloro substitution on the phenyl ring exhibited IC50 value of 0.007 μM better than other substitutions. Compounds 3n with 3-NO2 groups showed significant improvement in activity. Compound 3h with 3-CN group substitution on the phenyl ring exhibited intermediate potency in the series. Constitutively, 3j and 3k containing 3-hydroxy and 3,4-di hydroxy groups attached to phenyl ring showed decrease in activity compared to other derivatives of the series, attributed to the presence electron withdrawing group decrease the potency.

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