Studies toward the synthesis of novel MDM2 inhibitor candidates
by
Dilek, Fikrican, author.
Title
:
Studies toward the synthesis of novel MDM2 inhibitor candidates
Author
:
Dilek, Fikrican, author.
Personal Author
:
Dilek, Fikrican, author.
Physical Description
:
xii, 49 leaves: charts;+ 1 computer laser optical disc.
Abstract
:
Protein protein interactions are valuable targets to discover novel anticancer agents. One of these is the p53-MDM2 interaction. In one of these interaction MDM2 protein inhibits p53 protein and may cause cancer. New drugs that inhibit this interaction are important for the treatment of cancer. One class of these anticancer agents are morpholinone derivative. In this study, it is aimed to synthesize new morpholinone derivatives. (R)-2-amino-2-(4-chlorophenyl)acetic acid was used as starting material for the synthesis. The first step was a trityl protection of amine with trityl chloride. Trityl protected amino acid was first reduced to N-Trt amino alcohol with LiAlH4 then oxidized to aldehyde by using Dess-Martin periodinane. The resulting aldehyde was reacted with 3-chlorophenylmagnesium bromide. This part of the synthesis was performed successfully. Then addition of methyl fumarate to this Grignard product was studied by a coupling reagents such as HATU. All attempts were failed. Then trityl group was removed by TFA and successfully coupled with methyl fumarate by using HATU. All cyclization reactions in the presence of a base like hydroxide, alkoxide or NaH to form morpholinone skeleton was failed. The cyclization reaction with the potassim carbonate in alcohol was successful and the morpholinone skeleton was formed.
Subject Term
:
Chemical inhibitors
p53 protein
p53 antioncogene
Added Author
:
Çağır, Ali,
Added Corporate Author
:
İzmir Institute of Technology. Chemistry.
Added Uniform Title
:
Thesis (Master)--İzmir Institute of Technology:Chemistry.
İzmir Institute of Technology:Chemistry --Thesis (Master).
Electronic Access
:
Library | Material Type | Item Barcode | Shelf Number | Status |
---|
IYTE Library | Thesis | T002536 | QD501 .D576 2018 | Tez Koleksiyonu |
IYTE Library | Supplementary CD-ROM | ROM3679 | QD501 .D576 2018 EK.1 | Tez Koleksiyonu |