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Title: Design Synthesis and Evaluation of Indole Based Compounds as Putative Anticancer Agents
Researcher: Singla, Ramit
Guide(s): Jaitak, Vikas
Keywords: Breast cancer, estrogen receptor alpha, induced fit, indole, RT-PCR, Western blotting
University: Central University of Punjab
Completed Date: 11/09/2018
Abstract: In the course of efforts to develop new chemotherapeutic agent for targeting newlinebreast cancer, indole-benzimidazole, indole-xanthendione, indole-chromene newlinecarbonitrile and indole-dihydropyridine derivatives were computationally newlinedesigned and synthesized. All the compounds were first analyzed for antiproliferative newlineactivity using ER-and#945; responsive T47D breast cancer cells line and newlinecytotoxicity using hPBMC. Further, all the synthesized compounds were also newlineevaluated for ER-and#945; binding affinity. Lead compounds 5f and 8f of series 1 and newline2; 10e and 10f of series 3, 11c and 12d of series 4 and 5 were found to be newlinemost active at both cellular and receptor level hence were biologically newlineevaluated for gene expression studies for targeting ER-and#945;. Cell imaging newlineexperiment clearly suggest that compounds were able to cross cell membrane newlineand accumulate thus causing cytotoxicity. Semiquantitative RT-PCR and newlineWestern blotting experiments further supported that lead compounds altered newlinethe expression of mRNA and protein of ER-and#945;, thereby preventing the further newlinetransactivation and signaling pathway in T47D cells line. Structural newlineinvestigation from induced fit simulation study suggest that lead compounds newlinebinds in a conformation similar to bazedoxifene by extensive hydrogen bonding newlineand Van der Waals forces. All these results indicate that compounds 5f, 8f, newline10e, 10f, 11c and 12d represents new putative anticancer agents and can be newlineproved promising in the discovery of antiestrogens for the management of newlinebreast cancer. newline
Appears in Departments:Department of Pharmaceutical Sciences and Natural Products

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01_title.pdfAttached File39.5 kBAdobe PDFView/Open
02_certificate.pdf62.99 kBAdobe PDFView/Open
03_acknowledgement.pdf38.33 kBAdobe PDFView/Open
04_abstract.pdf95.01 kBAdobe PDFView/Open
05_table of contents.pdf207.01 kBAdobe PDFView/Open
06_list of tables.pdf23.34 kBAdobe PDFView/Open
07_list of figures.pdf76.97 kBAdobe PDFView/Open
08_list of schemes.pdf80.47 kBAdobe PDFView/Open
09_list of appendices.pdf20.31 kBAdobe PDFView/Open
10_list of abbreviations.pdf207.01 kBAdobe PDFView/Open
11_chapter 1.pdf661.52 kBAdobe PDFView/Open
12_chapter 2.pdf1.58 MBAdobe PDFView/Open
13_chapter 3.pdf543.86 kBAdobe PDFView/Open
14_chapter 4.pdf529.98 kBAdobe PDFView/Open
15_chapter 5.pdf2.09 MBAdobe PDFView/Open
16_chapter 6.pdf99.49 kBAdobe PDFView/Open
17_references.pdf257.31 kBAdobe PDFView/Open
18_appendices.pdf808.22 kBAdobe PDFView/Open

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