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Volume 8, Issue 2 (Suppl) Chem Sci J 2017
ISSN: 2150-3494 CSJ, an open access journal Euro Chemistry 2017
May 11-13, 2017
May 11-13, 2017 Barcelona, Spain
4th European Chemistry Congress
Jae-Sang Ryu, Chem Sci J 2017, 8:2(Suppl)
Synthesis of 1, 2, 3-triazole-linked salicylamide analogs as potent aurora kinase inhibitors
Jae-Sang Ryu
Ewha Womans University, Republic of Korea
The Aurora family is a member of the Ser/Thr protein kinases regulating mitosis. They includes Aurora A, B and C possessing
individual function and different cellular localization during cell cycle. An overexpression of Aurora A and B, which has been
observed in various tumor types, is known to connect to chromosomal instability, oncogenic transformation, and tumor progression.
Although Aurora kinase is considered as a promising therapeutic target in cancer and several Aurora inhibitors have currently reached
the clinical evaluation stage, Aurora-selective drug is not yet approved by FDA. Previously, we identified a potent antiproliferative
substance by constructing a small molecule library that mimics lavendustin, a natural kinase inhibitor, using a rapid 'click-fragment
assembly' and screeningmethod. Based on this lead compound, various 1,2,3-triazolylsalicylamide analogs were designed, synthesized
via Cu(I)-catalyzed azide–alkyne 1,3-dipolar cycloaddition (CuAAC) and evaluated biochemically for the Aurora kinase inhibitory
activities. Among twenty-four membered 1,2,3-triazole library, compound 8a exhibited much lower IC50 values against Aurora A
kinase than the lead compound, and compound 8m showed a nanomolar IC50 value against Aurora B. In this presentation, we
describe the design, synthesis, and biochemical evaluation of 1,2,3-Triazole-linked Salicylamide Analogs.
Biography
Jae-Sang Ryu has completed his PhD from Northwestern University, IL, USA and postdoctoral studies from Memorial Sloan-Kettering Cancer Center, NY, USA.
He is a profssor of college of Pharmacy & Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul, Korea. He has been searching for new
drug candidates based on disease mechanisms and combinatorial approaches. His lab is currently working on the development of allergic/anticancer drugs using
peptide libraries and natural compound-like compound libraries. He has published many papers in SCI international journals and applied for patents related to the
development of antiallergic drugs and anti-cancer drugs.