A new series of 3‐substituted 4‐(4‐methyloxy phenyl)‐1H‐pyrrole derivatives were synthesized and biologically evaluated for potential anticancer activity. Fifteen targeted compounds showed high selectivity toward normal cells and cancer cells: that is, all targeted compounds had no obvious cytotoxicity toward normal human cells (HUVEC and NIH/3T3), but some compounds exhibited broad‐spectrum proliferation inhibitory activity against the screened cancer cell lines. Among these pyrrole derivatives, compounds 3b and 3o showed potent anticancer activity against the MG‐63 cell line, with IC50
values of 14.9 and 12.7 μM, respectively. Other pyrrole derivatives also showed promising proliferation inhibitory activity, including compound 3d against A375 (IC50
= 18.6 μM), compound 3f and 3j against MGC80‐3 (IC50
= 19.9 μM), and compound 3o against MGC80‐3 (IC50
= 11.9 μM). Because the developed pyrrole derivatives showed strong anticancer activity and high selectivity, this new series of pyrrole derivatives could be considered as promising lead compounds for further development of potent and safe anticancer agents.
The aims of this paper are to investigate the inherent relationship between the structures of the polyacrylates and release behaviors as drug carriers in the transdermal drug delivery systems. Three model polyacrylates compounds were synthesized by radical polymerization. Three polymer materials were characterized by Fourier transform infrared, differential scanning calorimeter and cytotoxicity, and the release behaviors of drug molecules transporting through the polymers membranes were tested. Moreover, the effects of the polymers’ structures on the permeability were studied by molecular dynamic simulation. The simulation results showed that higher chains mobility and larger fractional free volume of the polymer membranes resulted in higher permeation rates. By comparing the monomers’ structure in the polymer materials, it was found that the polymer chains’ mobility decreases, and permeation rate correspondingly decreases with the increase in the amount and volume of side groups on the double bonds.
A film-like copolymer composed of 2-hydroxy-3-phenoxypropylacrylate, 4-hydroxybutyl acrylate and cyclohexyl methacrylate was synthesized and exploited as a rate-controlling membrane in the transdermal drug delivery systems (TDDs). A series of acrylate copolymers with different formulations were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry and tensile strength, and then evaluated by clonidine hydrochloride transporting through the films. It was found that the formulation M2 composed of three monomers at a ratio of 4:4:2 (w/w/w) showed excellent mechanical and permeation properties. The optimal formulation M2 was further characterized by scanning electron microscopy, contact angles and swelling ratio, and then the permeation behaviors of five different physicochemical drugs transporting through the M2 were evaluated. The results showed that the permeation behaviors were influenced by many factors including the thickness of the membrane, the physicochemical properties of the drugs, the dose of the drugs and the interactions between the drugs and the membrane. This type of copolymer membrane might open new applications in the field of TDDs.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.