Exact(3)
In comparison to control media, human HCM was significantly more potent (p = 0.029).
In mouse jejunum, Fp.Cr, caused a concentration-dependent (0.01-1 0.01-1 stimg/mlt effect with efficacy of 62 ± 3% being lestimulant (p < 0.05) than in mouseffectm.
In long-term oestrogen deprived (MCF7-X) resistant MCF-7 cells, RAD001 was found to be even less potent (P <0.05) with an IC50 >1 μM.
Similar(57)
A series of 1,4-substituted arylalkyl piperazine derivatives were synthesized and studied with the aim to obtain potent P-gp-dependent multidrug-resistant (MDR) reversers.
Among them, the most potent compound 4 showed a comparable activity with the known potent P-gp inhibitor WK-X-34 with lower cytotoxicity toward K562 cells (IC50 >100 μM).
Compounds 12c with a Y-shaped scaffold, and compound 17c which is 'X-shaped' scaffold and possesses a 4-diethylamino group at aryl ring B, turned out to be the most potent P-gp modulators.
In a continuing search for potent P-gp-dependent multidrug-resistant (MDR) reversers we synthesized and studied a new series of N-alkanol-N-cyclohexanol amine aryl esters characterized by the presence of two linkers with different flexibility: a polymethylene chain of variable length and a cyclohexylic scaffold, that gave origin to two geometrical isomers (cis and trans).
Following the identification of a novel polycyclic scaffold, leading to the previously reported potent P-gp modulator 1, a small series of easily affordable derivatives bearing a properly selected nitrogen-containing but-2-ynyl side chain was now synthesized and tested to evaluate the MDR reverting activity on two different experimental models.
This concept is strengthened by the finding that fucoidan fractions act as a potent P-selectin inhibitor [2].
To analyze whether P-gp inhibition compromises parasite invasion, we blocked P-gp function in isolated parasites with GF120918, a potent P-gp inhibitor of the latest generation [13].
Here we investigated the effects of the potent P-gp inhibitor GF120918 in the biology of Toxoplasma gondii, a model intracellular parasite and an important human pathogen, causing toxoplasmosis.
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