TAILIEUCHUNG - Summary of Chemistry doctoral thesis: Synthesis and evaluation of anticancer activity of tubulysin derivatives

Synthesis of several derivatives and tubulysin analogues with the replacement of the amino acid methylpipecolic (Mep) at the N-terminal, replacing N,O-acetyl group by methyl group, and researching the role of tubuphenylalanine (Tup) group at the C-terminal . | MINISTRY OF EDUCATION VIETNAM ACADEMY AND TRAINING OF SCIENCES AND TECHNOLOGY GRADUATE UNIVERSITY OF SCIENCE AND TECHNOLOGY ----------------------------- LE VAN HAI SYNTHESIS AND EVALUATION OF ANTICANCER ACTIVITY OF TUBULYSIN DERIVATIVES Major Organic Chemistry Code SUMMARY OF CHEMISTRY DOCTORAL THESIS HA NOI 2020 The thesis was completed at Institute of Chemistry Vietnam Academy of Science and Technology Supervisor 1. Asso. Prof. Dr. Tran Van Loc Institute of Chemistry-Vietnam Academy of Science and Technology 2. Dr. Tran Van Chien Institute of Chemistry-Vietnam Academy of Science and Technology Reviewer 1 Reviewer 2 Reviewer 3 The thesis will be presented in front of the doctoral thesis council at Graduate University of Science and Technology - Vietnam Academy of Science and Technology- 18 Hoang Quoc Viet Road Cau Giay Hanoi. At time . The thesis can be found at - Library of Academy of Science and Technology - National Library of Vietnam OPENING 1. The essential of the thesis The natural compounds have considered infinite supplies of bioactive substances for research and medical application. The abundance and diversity of the substance-frames had highly bioactive. Especially the mechanism of action of each layer of these frames attracted of researchers so far. For the purpose of research on drug development compounds from microbial sources are often achieved by total synthesis or will be modified in chemical structure to create large quantities of products as well as new derivatives. Tubulysins are the tetrapeptide class figure isolated from two myxobacteria strains Angiococcus disciformis An d48 and Archangium gephyra Ar 315. Studies have shown that tubulysins are the best class of anticytokines known to nowaday. The cancer cell inhibitory of tubulysins are show a wide range of human cancer cell lines such as ovarian cancer breast cancer prostate cancer colon lung and blood cancer. In vitro and in vivo studies have shown that tubulysins inhibit .

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