1239028-27-3Relevant academic research and scientific papers
New clicked full agonists of the estrogen receptor β
Demkowicz, Sebastian,Filipiak, Kamila,Maslyk, MacIej,Ciepielski, Jakub,De Pascual-Teresa, Sonia,Martin-Santamaria, Sonsoles,De Pascual-Teresa, Beatriz,Ramos, Ana
, p. 3697 - 3706 (2013/04/10)
A click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists for ERβ at a 20 μM concentration, and one of them (3c) showed no proliferative effect on MCF-7 cells.
A rapid synthesis of lavendustin-mimetic small molecules by click fragment assembly
Yoon, Jieun,Ryu, Jae-Sang
supporting information; experimental part, p. 3930 - 3935 (2010/08/20)
Lavendustin-mimetic small molecules modifying the linker -CH 2-NH- with an 1,2,3-triazole ring have been synthesized via a click chemistry. Two pharmacophoric fragments of lavendustin were varied to investigate chemical space and the auxophoric -CH2-NH- was altered to an 1,2,3-triazole for rapid click conjugation. The small molecules were evaluated against HCT116 colon cancer and CCRF-CEM leukemia cell lines. Among 28 analogues, 3-phenylpropyl ester 26b inhibited CCRF-CEM leukemia cell growth with GI50 value of 0.9 μM.
