777075-10-2Relevant academic research and scientific papers
Antiproliferative activity of Rhinacanthus nasutus (L.) KURZ extracts and the active moiety, rhinacanthin C
Gotoh, Akinobu,Sakaeda, Toshiyuki,Kimura, Takashi,Shirakawa, Toshiro,Wada, Yoshitaka,Wada, Atsushi,Kimachi, Tetsutaro,Takemoto, Yoshiji,Iida, Akira,Iwakawa, Seigo,Hirai, Midori,Tomita, Hisako,Okamura, Noboru,Nakamura, Tsutomu,Okumura, Katsuhiko
, p. 1070 - 1074 (2004)
Rhinacanthus nasutus (L.) KURZ (Acanthaceae) is a shrub widely distributed in South China and India. In this study, the antiproliferative activity of the ethanol extract of root and aqueous extract of leaves of R. nasutus, and the supposed active moiety rhinacanthin C was assessed in vitro using the human cervical carcinoma cell line HeLa, its MDR1-overexpressing subline Hvr100-6, human prostate carcinoma PC-3 cells and human bladder carcinoma T24 cells. Rhinacanthin C was chemically synthesized and its content in the R. nasutus extracts was determined by HPLC with a photodiode array detector. The antiproliferative activity of the R. nasutus extracts was also assessed in vivo using sarcoma 180-bearing mice. It was suggested that 1) the in vitro antiproliferative activity of rhinacanthin C was comparable with or slightly weaker than that of 5-FU, 2) rhinacanthin C showed antiproliferative activity for MDR1-overexpressing Hvr100-6 cells, similarly to parent HeLa cells, 3) the in vitro antiproliferative activity of the ethanol extract of root R. nasutus was due to rhinacanthin C, whereas that of the aqueous extract of leaves of R. nasutus was due to constituents other than rhinacanthin C, and 4) both of the R. nasutus extracts showed in vivo antiproliferative activity after oral administration once daily for 14 d.
An Efficient and Reliable Catalyst System Using Hemilabile Aphos for B-Alkyl Suzuki-Miyaura Cross-Coupling Reaction with Alkenyl Halides
Ye, Ning,Dai, Wei-Min
, p. 831 - 835 (2013/03/29)
The 9-methoxy-9-borabicyclo[3.3.1]nonane-based B-alkyl Suzuki-Miyaura cross-coupling reaction (the 9-MeO-9-BBN variant) has been efficiently performed by using the catalyst consisting of Pd(OAc)2 and a hemilabile P,O-ligand, Aphos-Y, under mild reaction conditions (K3PO 4·3H2O, THF/H2O, room. temp.). For applications in the total synthesis of structurally complex natural products, the Johnson protocol commonly uses two ligands (dppf and Ph3As) and two organic solvents (THF and DMF). In contrast, the new version reported here employs one ligand (Aphos-Y) and one organic solvent (THF). Moreover, the broad substrate scope and the excellent functional group tolerance of the Pd(OAc) 2-Aphos-Y catalyst have been demonstrated, providing a reliable and simple synthetic tool for fragment coupling in total synthesis through formation of a C(sp3)-C(sp2) bond. Copyright
