Synthesis and biological evaluation of biaryl compounds as PD-L1 and c-MYC inhibitors
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Title
Synthesis and biological evaluation of biaryl compounds as PD-L1 and c-MYC inhibitorsAuthor (s)
Tutor/Supervisor; University.Department
Carda Usó, Pedro Miguel; Universitat Jaume I. Departament de Química Inorgànica i OrgànicaDate
2018-07Publisher
Universitat Jaume IAbstract
The main aim of this project is the search for compounds with dual inhibitory activity on cMYC and PD-L1.
Following the recent publication focused on the use of biaryl derivatives as small-molecule
inhibitors of ... [+]
The main aim of this project is the search for compounds with dual inhibitory activity on cMYC and PD-L1.
Following the recent publication focused on the use of biaryl derivatives as small-molecule
inhibitors of cancer-related proteins, the research group I have worked with is carrying out a line
of research on the development of derivatives of arylpyridines and arylpyrimidines as chemical
inhibitors of c-MYC and PD-L1 proteins. Therefore, it has been decided to synthesize
(methoxyphenyl)pyridine and (methoxyphenyl)pyrimidine derivative compounds because
previous results obtained within the research group showed that similar biaryl derivatives had
significant inhibitory activity on PD-L1 and c-MYC.
Thus, the aims of this project are:
1. Synthesis of the biaryl compounds depicted in Figure 12.
2. Biologic evaluation of the selected compounds:
2.1. Study of the antiproliferative activity and cytotoxicity by MTT assay.
2.2. Study of the interaction of compounds with PD-L1 by Protein Thermal Shift assay.
2.3. Study of the effect on c-MYC and PD-L1 in tumor cells by flow cytometry assay.
2.4. Cell co-cultures assays. [-]
Description
Treball Final de Grau en Química. Codi: QU0943. Curs acadèmic: 2017/2018
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- Grau en Química [265]