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|Title:||NOVEL 2 4 THIAZOLIDINEDIONE ANALOGUES AS CYTOTOXIC AGENTS DESIGN DOCKING STUDY SYNTHESIS AND BIOLOGICAL EVALUATION|
|Researcher:||Shah Dhaval Girishbhai|
|Abstract:||Novel 2,4-Thiazolidinedione derivatives were synthesized through reaction of N-benzoyl substituted aryl alkyl halide with N-substituted 2,4-thiazolidinedione derivatives and screened for their in vitro cytotoxic activity by MTT assay. The cell lines used were MCF 7 (Breast cancer cell), HELA (Cervical cancer cell line), HEK (Normal epidermal kidney cell line) HEP (Laryngeal cancer cell line) MDA MB 468 (Brest cancer cell line). Result of screening on cell line showed moderate to good cytotoxic activity for all the compounds. 2,4-thiazolidinedione moiety with Chloride substitution at 4th position having IC50 = 3.63 and#956;M on HEP cell line and IC50 = 1.07 and#956;M on HEK cell line while 2 chloride substitution on 2nd and 3rd position having IC50 = 1.09 and#956;M on HELA cell line, IC50 = 1.989 and#956;M on M468 cell line and IC50 = 2.5 and#956;M on MCF7 cell line was found to be most active compared to standard Methotrexate (IC50 = 0.22 and#956;M HEP, IC50 =0.072 and#956;M HEK, IC50 = 0.102 and#956;M HELA, IC50 = 0.152 and#956;M M468, IC50 = 0.100 and#956;M MCF7 ). Structure Activity Relationship of synthesized analogs suggested that the attachment of electron withdrawing groups like Chloro at R-2 position and Acetyl group at R-1 shows better cytotoxic activity. Activity by hydrogen and acetyl substitution at R1 position linked with N substituted 2,4 - Thiazolidinedione scaffold give better activity in the order of H gt CH2COOH. The findings may impart new direction to medicinal chemists and biochemists for further investigations of 2,4- Thiazolidinedione containing cytotoxic agents. newline|
|Appears in Departments:||FACULTY OF PHARMACY|
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