125818-00-0Relevant articles and documents
New 1,2,4-oxadiazole nortopsentin derivatives with cytotoxic activity
Cascioferro, Stella,Attanzio, Alessandro,Di Sarno, Veronica,Musella, Simona,Tesoriere, Luisa,Cirrincione, Girolamo,Diana, Patrizia,Parrino, Barbara
, (2019/01/14)
New analogs of nortopsentin, a natural 2,4-bis(30-indolyl)imidazole alkaloid, in which the central imidazole ring of the natural lead was replaced by a 1,2,4-oxadiazole moiety, and in which a 7-azaindole portion substituted the original indole moiety, were efficiently synthesized. Among all derivatives, prescreened against the HCT-116 colon rectal carcinoma cell line, the two most active compounds were selected and further investigated in different human tumor cells showing IC50 values in the micromolar and submicromolar range. Flow cytometric analysis of propidium iodide-stained MCF-7 cells demonstrated that both the active derivatives caused cell cycle arrest in the G0-G1 phase. The cell death mechanism induced by the compounds was considered to be apoptotic by measuring the exposure of phosphatidylserine to the outer membrane and observed morphological evaluation using acridine orange/ethidium bromide double staining. Moreover, further tested on intestinal normal-like differentiated Caco-2 cell line, they exhibited preferential toxicity towards cancer cells.
SYNTHESIS OF FUNCTIONAL DERIVATIVES OF INDOLE-3-CARBOXYLIC ACIDS
Kelarev, V. I.,Gasanov, S. Sh.,Karakhanov, R. A.,Polivin, Yu. N.,Kuatbekova, K. P.,Panina, M. E.
, p. 2069 - 2074 (2007/10/02)
Methods are described for the synthesis of the esters, hydrazides, amidines, N-phenylamidines, N1-phenylamidrazones, N1-acylamidrazones, and amide oximes of indole-3-carboxylic and 1-methylindole-3-carboxylic acids.
