Design, synthesis and biological evaluation of 2-pyrrolone derivatives as radioprotectors

Satoh, Hidetoshi; Ochi, Shintaro; Mizuno, Kenta; Saga, Yoshitaka; Ujita, Shohei; Toyoda, Miyu; Nishiyama, Yuichi; Tada, Kasumi; Matsushita, Yosuke; Deguchi, Yuichi; Suzuki, Keiji; Tanaka, Yoshimasa; Ueda, Hiroshi; Inaba, Toshiya; Hosoi, Yoshio; Morita, Akinori; Aoki, Shin

doi:10.1016/j.bmc.2022.116764

Search citation statements

Order By: Relevance

Paper Sections

Select...

Introduction1

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2022

Publication Types

Select...

Article1

Relationship

Self Cite0

Independent1

Authors

Journals

Cited by 1 publication

(1 citation statement)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The pyrrolin‐2‐one scaffold is present in a range of natural products and pharmaceuticals, most of these displaying interesting biological activities (Figure 1), [1] e. g., I (antiviral), [2] II (against Plasmodium falciparum K1), [3] III (anti‐apoptotic), [4] IV (antitumoral), [5] V (antibiotic), [6] VI (electron acceptor and fluorescent probe), [7] VII (antibacterial) [8] and VIII (neurotrophic properties) [9] . A promising approach for synthesis of pharmaceutically and biologically active pyrrolin‐2‐ones, has been rarely explored due to their poor synthetic accessibility.…”

Section: Introductionmentioning

confidence: 99%

Ugi Cascade Sequence for the Construction of 3‐Pyrrolin‐2‐one Scaffolds: Anti‐proliferation in Prostate Cancer Cells

Lei

Yang

et al. 2022

Chemistry An Asian Journal

View full text Add to dashboard Cite

Herein, a small series of 3-pyrrolin-2-ones was efficiently synthesized through a three-step Ugi cascade sequence. This method features readily available substrates, simple aqueous workup procedures and good yields, dramatically improving generality of reaction. Importantly, the newly product N-benzyl-2-(3-(4-chlorophenyl)-4-methyl-2-oxo-2,5dihydro-1H-pyrrol-1-yl)-2-phen-ylacetamide exhibited potent anti-proliferation in prostate cancer cell line through G1/S cell cycle arrest and targeted in PI3K/AKT/TSC2 signal pathway.

show abstract