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Researcher: Ravani Rasikkumar Meghjibhai
Guide(s): L.J.Patel
University: Ganpat University
Completed Date: 2017
Abstract: Synthesis of novel quinazoline derivatives was performed from reaction of N-benzoyl substituted piperazine-1-carbothioamide with 4-(2-chlormethyl) quinazoline-4-yloxy phenyl benzamide derivatives and screened for their in vitro cytotoxic activity by MTT assay. Docking study was performed for selection of best scored compound for synthesis based on minimized energetic compounds. The cell lines used were MCF 7 (Breast cancer cell), HCT 15 (Colon cancer cell line), and VERO (Normal epidermal kidney cell). Result of screening on cell line showed moderate to good cytotoxic activity for all the compounds. Compound GNU 02 (IC50 = 7.94 and#956;M, MCF), GNU 12 (IC50 = 8.43 and#956;M, HCT) and GNU 25 (IC50 = 9.41 and#956;M, HCT) was found to be most active compared to standard gefitinib (IC50 = 1.51 and#956;M HCT, IC50 =22.37 and#956;M MCF). Pharmacokinetic study was done based on computer software Molinspiration programme and proved best absorption, Distribution, Metabolism and Excretion profile of synthesized compounds. Some compounds which are not follow drug likeliness can developed by formulation development. Structure activity relationship of synthesized analogs suggested that the attachment of electron withdrawing groups like Nitro, Chloro gave better cytotoxic activity then unsubstituted phenyl and electron donating groups. Activity by substituted piperazine at 2nd position of thiazole linked with quinazoline scaffold gave better activity in the order of H gt CH3 gt C6H5. Our findings may impart new direction to medicinal chemists and biochemists for further investigations of quinazoline-thiazole containing cytotoxic agents. newline
Appears in Departments:FACULTY OF PHARMACY

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10 list of table.pdfAttached File13.02 kBAdobe PDFView/Open
11 abstract.pdf94.26 kBAdobe PDFView/Open
12. list of abbrevation.pdf73.76 kBAdobe PDFView/Open
13. introduction.pdf394.57 kBAdobe PDFView/Open
14. literature.pdf167.01 kBAdobe PDFView/Open
15. aim of work.pdf66.61 kBAdobe PDFView/Open
16. design of target molecule.pdf78.39 kBAdobe PDFView/Open
17. material.pdf67.41 kBAdobe PDFView/Open
18. docking.pdf871.62 kBAdobe PDFView/Open
19 experimental work.pdf272.67 kBAdobe PDFView/Open
1.emboss.pdf37.19 kBAdobe PDFView/Open
20. result and discussion.pdf1.25 MBAdobe PDFView/Open
21. summary and conclusion.pdf66.89 kBAdobe PDFView/Open
22. references.pdf125.87 kBAdobe PDFView/Open
23 publication.pdf65.9 kBAdobe PDFView/Open
26. seperator pages.pdf55 kBAdobe PDFView/Open
2.certificate.pdf12.01 kBAdobe PDFView/Open
3.certificate 2.pdf33.63 kBAdobe PDFView/Open
4.declaration.pdf33.37 kBAdobe PDFView/Open
5.thesis approval sheet.pdf22.22 kBAdobe PDFView/Open author.pdf19.61 kBAdobe PDFView/Open
7. aknowledgement.pdf39.98 kBAdobe PDFView/Open
8 index.pdf81.42 kBAdobe PDFView/Open
9 list of figure.pdf34.06 kBAdobe PDFView/Open

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