1214741-31-7Relevant academic research and scientific papers
Concise synthesis of catechin probes enabling analysis and imaging of EGCg
Yoshida, Atsushi,Hirooka, Yasuo,Sugata, Yusuke,Nitta, Mariko,Manabe, Tamiko,Ido, Shunsuke,Murakami, Kouki,Saha, Repon Kumer,Suzuki, Takashi,Ohshima, Motohiro,Yoshida, Akira,Itoh, Kunihiko,Shimizu, Kosuke,Oku, Naoto,Furuta, Takumi,Asakawa, Tomohiro,Wakimoto, Toshiyuki,Kan, Toshiyuki
, p. 1794 - 1796 (2011)
A concise synthesis of APDOEGCg (3) was accomplished. Due to the reactivity of its amine group, the compound could be easily converted to the fluorescein probe 21 and immunogen probe 22 efficiently. We then demonstrated the usefulness of the probes for im
Discovery and SAR of Natural-Product-Inspired RXR Agonists with Heterodimer Selectivity to PPARδ-RXR
Nakashima, Ken-Ichi,Yamaguchi, Eiji,Noritake, Chihaya,Mitsugi, Yukari,Goto, Mayuki,Hirai, Takao,Abe, Naohito,Sakai, Eiji,Oyama, Masayoshi,Itoh, Akichika,Inoue, Makoto
, p. 1526 - 1534 (2020/05/19)
A known natural product, magnaldehyde B, was identified as an agonist of retinoid X receptor (RXR) α. Magnaldehyde B was isolated from Magnolia obovata (Magnoliaceae) and synthesized along with more potent analogs for screening of their RXRα agonistic activities. Structural optimization of magnaldehyde B resulted in the development of a candidate molecule that displayed a 440-fold increase in potency. Receptor-ligand docking simulations indicated that this molecule has the highest affinity with the ligand binding domain of RXRα among the analogs synthesized in this study. Furthermore, the selective activation of the peroxisome proliferator-activated receptor (PPAR) δ-RXR heterodimer with a stronger efficacy compared to those of PPARα-RXR and PPARγ-RXR was achieved in luciferase reporter assays using the PPAR response element driven reporter (PPRE-Luc). The PPARδactivity of the molecule was significantly inhibited by the antagonists of both RXR and PPARδ, whereas the activity of GW501516 was not affected by the RXR antagonist. Furthermore, the molecule exhibited a particularly weak PPARδagonistic activity in reporter gene assays using the Gal4 hybrid system. The obtained data therefore suggest that the weak PPARδagonistic activity of the optimized molecule is synergistically enhanced by its own RXR agonistic activity, indicating the potent agonistic activity of the PPARδ-RXR heterodimer.
Oxidative spirocyclization of phenolic sulfonamides: Scope and applications
Liang, Huan,Ciufolini, Marco A.
supporting information; experimental part, p. 13262 - 13270 (2011/03/17)
A full account of the oxidative dearomatization of para- and ortho-phenolic sulfonamides is provided together with an overview of the chemistry of the products and their elaboration to building blocks for spirocyclic alkaloids. A concise total synthesis of putative lepadiformine complements the discussion. Making building blocks: The oxidative dearomatization of para- and ortho-phenolic sulfonamides provides building blocks for spirocyclic alkaloids (see scheme). The chemistry of the products of this reaction and a concise total synthesis of putative lepadiformine is given.
