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Jae-Sang Ryu

Ewha Womans University, Republic of Korea

Title: Synthesis of 1,2,3-Triazole-linked salicylamide analogs as potent aurora kinase inhibitors

Biography

Biography: Jae-Sang Ryu

Abstract

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 screening method. 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.