1387590-73-9Relevant academic research and scientific papers
3-Phenylalkyl-2H-chromenes and -chromans as novel rhinovirus infection inhibitors
Conti, Cinzia,Proietti Monaco, Luca,Desideri, Nicoletta
, p. 2074 - 2083 (2017)
Following our studies on structure-activity relationships of anti-rhinovirus chromene and chroman derivatives, we designed and synthesized new series of 3-phenylalkyl-2H-chromenes and -chromans bearing differently sized, aliphatic linker chains between the two cycles. The cytotoxicity and the antiviral activity of the new compounds on human rhinovirus (HRV) serotype 1B and 14 infection were evaluated in HeLa cell cultures. Most of the tested compounds interfered with HRV1B multiplication in the micromolar or submicromolar concentrations while HRV14 was less susceptible. 3-[3-(4-Chlorophenyl)propyl]chroman (9c) was selected for preliminary mechanism of action studies due to its potent activity against both serotypes (IC50 of 0.48?μM and 1.36?μM towards HRV1B and 14, respectively) coupled with high selectivity (SI?=?206.18 and 73.26, respectively). Results of time of addition/removal studies suggest that 9c, similarly to related derivatives, behaves as a capsid binder interfering with some early events of the HRV1B infectious cycle.
An atom-economical approach to the synthesis of potentially bioactive 2 H-chromenes via CuI-catalyzed reactions of Alkyl/Aryl-(E)-(o-propargyloxy)styryl ketones
Majumdar,Ansary, Inul,Shyam, Pranabk.,Roy
, p. 1225 - 1229 (2012/06/04)
A series of potentially bioactive 2H-chromenes have been synthesized in good yields (60-82%) via CuI-catalyzed reactions of alkyl/aryl-(E)-(o- propargyloxy)styryl ketones in an atom-economical approach. Georg Thieme Verlag Stuttgart · New York.
