Design, Synthesis and Evaluation of Indole Based Compounds as Putative Anticancer Agents

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dc.contributor.authorSingla, Ramit
dc.contributor.supervisorJaitak, Vikas
dc.date.accessioned2020-08-21T06:36:34Z
dc.date.accessioned2024-08-13T12:05:05Z
dc.date.available2020-08-21T06:36:34Z
dc.date.available2024-08-13T12:05:05Z
dc.date.issued2018
dc.description.abstractIn the course of efforts to develop new chemotherapeutic agent for targeting breast cancer, indole-benzimidazole, indole-xanthendione, indole-chromene carbonitrile and indole-dihydropyridine derivatives were computationally designed and synthesized. All the compounds were first analyzed for antiproliferative activity using ER-α responsive T47D breast cancer cells line and cytotoxicity using hPBMC. Further, all the synthesized compounds were also evaluated for ER-α binding affinity. Lead compounds 5f and 8f of series 1 and 2; 10e and 10f of series 3, 11c and 12d of series 4 and 5 were found to be most active at both cellular and receptor level hence were biologically evaluated for gene expression studies for targeting ER-α. Cell imaging experiment clearly suggest that compounds were able to cross cell membrane and accumulate thus causing cytotoxicity. Semiquantitative RT-PCR and Western blotting experiments further supported that lead compounds altered the expression of mRNA and protein of ER-α, thereby preventing the further transactivation and signaling pathway in T47D cells line. Structural investigation from induced fit simulation study suggest that lead compounds binds in a conformation similar to bazedoxifene by extensive hydrogen bonding and Van der Waals forces. All these results indicate that compounds 5f, 8f, 10e, 10f, 11c and 12d represents new putative anticancer agents and can be proved promising in the discovery of antiestrogens for the management of breast cancer.en_US
dc.identifier.accessionnoT00867
dc.identifier.citationSingla, Ramit & Jaitak, Vikas (2018) Design, Synthesis and Evaluation of Indole Based Compounds as Putative Anticancer Agentsen_US
dc.identifier.urihttp://10.2.3.109/handle/32116/2742
dc.language.isoen_USen_US
dc.publisherCentral University of Punjaben_US
dc.subjectBreast canceren_US
dc.subjectestrogen receptor alphaen_US
dc.subjectinduced fiten_US
dc.subjectindoleen_US
dc.subjectRT-PCRen_US
dc.subjectWestern blottingen_US
dc.titleDesign, Synthesis and Evaluation of Indole Based Compounds as Putative Anticancer Agentsen_US
dc.typeThesisen_US

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