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, Türkiye, 10 - 13 Mart 2022, ss.54-58

  • Yayın Türü: Bildiri / Tam Metin Bildiri
  • Basıldığı Şehir: Antalya
  • Basıldığı Ülke: Türkiye
  • Sayfa Sayıları: ss.54-58
  • Van Yüzüncü Yıl Üniversitesi Adresli: Evet

Özet 

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.