Structural Approach Into The Design of Potent Anticancer Indole-Oxazole Derivatives via Tubulin Polymerization Inhibition


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Kuzu B.

International 10. Drug Chemistry Congress, Antalya, Turkey, 10 - 13 March 2022, pp.54-58

  • Publication Type: Conference Paper / Full Text
  • City: Antalya
  • Country: Turkey
  • Page Numbers: pp.54-58
  • Van Yüzüncü Yıl University Affiliated: Yes

Abstract

Microtubules are composed of α-β-tubulin heterodimers, and drugs that interfere with microtubule dynamics are widely used in cancer chemotherapy. Small synthetic molecules containing an indole core have been identified as microtubule inhibitors and reported to be used as anticancer agents. In this study, strategic design, synthesis and tubulin polymerization inhibitor potentials of indole-oxazole ring systems were investigated. It was determined from the docking study that the designed compounds would exhibit tubulin polymerization by acting on the colchicine binding site. In addition, theoretical pharmacokinetic studies of target compounds were performed. The results of docking and theoretical ADMET studies show that the designed compounds will be potential anticancer agents via tubulin polymerization.