2948-15-4Relevant articles and documents
Synthesis and biological evaluation of phenstatin metabolites
Ghinet, Alina,Rigo, Beno?t,Hénichart, Jean-Pierre,Le Broc-Ryckewaert, Delphine,Pommery, Jean,Pommery, Nicole,Thuru, Xavier,Quesnel, Bruno,Gautret, Philippe
supporting information; experimental part, p. 6042 - 6054 (2011/11/29)
Previous investigations on the incubation of phenstatin with rat and human microsomal fractions revealed the formation of nine main metabolites. The structures of eight of these metabolites have been now confirmed by synthesis and their biological properties have been reported. Eaton's reagent was utilized as a convenient condensing agent, allowing, among others, a simple multigram scale preparation of phenstatin. Synthesized metabolites and related compounds were evaluated for their antiproliferative activity in the NCI-60 cancer cell line panel, and for their effect on microtubule assembly. Metabolite 23 (2′-methoxyphenstatin) exhibited the most potent in vitro cytotoxic activity: inhibition of the growth of K-562, NCI-H322M, NCI-H522, KM12, M14, MDA-MB-435, NCI/ADR-RES, and HS 578T cell lines with GI50 values 50 = 3.2 μM vs 15.0 μM) and induced G2/M arrest in murine leukemia DA1-3b cells. The identification of this active metabolite led to the design and synthesis of analogs with potent in vitro cytotoxicity and inhibition of microtubule assembly.
Environmentally friendly methods for syntheses of new aromatic bisesters
Zbancioc, Gheorghita N.,Zbancioc, Ana Maria V.,Mangalagiu, Ionel I.
experimental part, p. 2201 - 2208 (2010/09/30)
Two environmentally friendly methods, one in liquid and the other in solid phase, for preparation of phenyl bisesters (bearing alkylating groups) under microwave (MW) irradiation are presented. The MW remarkably enhanced the rate of acceleration for ester