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

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

JOURNAL=Frontiers in Chemistry

VOLUME=10

YEAR=2022

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2022.975559

DOI=10.3389/fchem.2022.975559

ISSN=2296-2646

ABSTRACT=<p>We have synthesized Rhopaladins’ analog (2<italic>E</italic>,4<italic>E</italic>)-4-chlorobenzylidene-2-(4-chlorostyryl)-<italic>N</italic>-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 (<italic>E</italic>)-<italic>N</italic>-(<italic>tert</italic>-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.</p>