Anticancer 5-arylidene-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones as tubulin inhibitors

Arch Pharm (Weinheim). 2022 Dec;355(12):e2200419. doi: 10.1002/ardp.202200419. Epub 2022 Sep 15.

Abstract

Studying the anticancer activity of 5-arylidene-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones towards cell lines of different cancer types allowed the identification of hit-compounds inhibiting the growth of daunorubicin- (CEM-DNR, IC50 = 0.32-1.28 µM) and paclitaxel-resistant (K562-TAX, IC50 = 0.21-1.23 µM) cell lines, with favorable therapeutic indexes. The studied compounds induced apoptosis and cellular proliferation in treated CCRF-CEM cells. The hit compounds were shown to induce mitotic arrest by interacting with tubulin, inhibiting its polymerization by binding to the colchicine binding site.

Keywords: 2-aminothiazol-4(5H)-ones; anticancer activity; tubulin inhibitors.

MeSH terms

  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Apoptosis
  • Binding Sites
  • Cell Line, Tumor
  • Cell Proliferation
  • Drug Screening Assays, Antitumor
  • Structure-Activity Relationship
  • Tubulin / metabolism
  • Tubulin Modulators* / chemistry
  • Tubulin Modulators* / pharmacology

Substances

  • Tubulin Modulators
  • Antineoplastic Agents
  • Tubulin