Frontiers in Chemistry (Aug 2022)

Green synthesis, structure optimization and biological evalution of Rhopaladins’ analog 2–styryl–5-oxopyrrolidine-2- carboxamide RPDPRH on CaSki cells

  • Li-Na Ke,
  • Li-Na Ke,
  • Ling-Qi Kong,
  • Ling-Qi Kong,
  • Xiu-Lian Zhu,
  • Feng-Xu Wu,
  • Qin-Hua Chen,
  • Bin Li,
  • Yun Dong,
  • Yun Dong,
  • Hong-Mei Wang,
  • Hong-Mei Wang,
  • Xiao-Hua Zeng,
  • Xiao-Hua Zeng

DOI
https://doi.org/10.3389/fchem.2022.975559
Journal volume & issue
Vol. 10

Abstract

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We have synthesized Rhopaladins’ analog (2E,4E)-4-chlorobenzylidene-2-(4-chlorostyryl)-N-cyclohexyl-1-(4-fluorophenyl)-5-oxopyrrolidine-2-carboxamide (RPDPRH) via a highly facile, inexpensive and green approach and verified the structural superiority of compound RPDPRH through molecular docking. Moreover, we further detected the anti-proliferation, apoptosis and HPV E6/E7 effects of RPDPRH on CaSki cells. Finally, we confirmed that compared with the previous compound (E)-N-(tert-butyl)-2-(4-chlorobenzoyl)-4-(4-fluorobenzylidene)-1-isopropyl-5-oxopyrrolidine-2-carboxamide (RPDPB), RPDPRH could better inhibit proliferation, induce apoptosis, and down-regulate HPV E6/E7 mRNA expression on Caski cells. And preliminary RT-PCR experiments have demonstrated that RPDPRH also could affect the expression of Bcl-2, Bax and Caspase-3 mRNA in Caski cells. In summary, RPDPRH has potential as an effective agent against cervical cancer and will play an important role in our subsequent research.

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