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Chemical Compound Review:

AC1MIOC4 (2R)-3-[2-(3,4- dimethoxyphenyl)-1,3...

Synonyms: AG-E-17384, LS-63132, CTK4D2849, Ro 44-5911, 168037-92-1

Eliason, J.F. et al., Eliason, J.F. et al., Abderrabi, M. et al.

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High impact information on Ro 44-5911

In a preliminary pharmacokinetic investigation, Ro 44-5912 appeared to have a longer half-life in mice than did its (R) enantiomer Ro 44-5911 (3.15 +/- 0.02 h versus 2.15 +/- 0.14 h) as measured by total radiolabel in plasma [1].
In an assay using the P-glycoprotein over-expressing cell line KB-8-5, the most active analogues for decreasing vincristine resistance were the racemate Ro 11-5160 and its two enantiomers, Ro 44-5911 (R) and Ro 44-5912 (S) [2].
Comparative in vitro evaluation of dithiane analogs of tiapamil, Ro 11-2933, Ro 44-5911 and Ro 44-5912 as multidrug resistance modulators [3].

References

The dithiane Ro 44-5912 enhances vinblastine sensitivity of drug resistant and parental KB lines in vivo. Eliason, J.F., Sawada, R., Tsukaguchi, T., Kobayashi, K., Ichihara, S., Konishi, C., Horii, I., Kuruma, I., Ramuz, H. Eur. J. Cancer (1995) [Pubmed]
Novel dithiane analogues of tiapamil with high activity to overcome multidrug resistance in vitro. Eliason, J.F., Ramuz, H., Yoshikubo, T., Ishikawa, T., Yamamoto, T., Tsuruo, T. Biochem. Pharmacol. (1995) [Pubmed]
Comparative in vitro evaluation of dithiane analogs of tiapamil, Ro 11-2933, Ro 44-5911 and Ro 44-5912 as multidrug resistance modulators. Abderrabi, M., Marchal, S., Merlin, J.L. Anticancer Drugs (1996) [Pubmed]

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