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Chemical Compound Review:

AG-I-00045 N-[2-(3,4- dimethoxyphenyl)ethyl]-N- methyl...

Synonyms: KST-1A9421, AC1L3GQN, CTK5H9997, AR-1B7205, AC1Q7FW2, ...

Mazzoni, A. et al., Mazzoni, A., Kyle, D.E. et al., Eliason, J.F. et al., Abderrabi, M. et al.

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Disease relevance of N-(3,4-Dimethyloxyphenethyl)-N-methyl-2-(2-naphthyl)-1,3-dithiane-2-propylamine

The ability of RO 11-2933 to modulate in vivo Doxorubicin and Cisplatin antitumor activity has been evaluated in sensitive and resistant P388 and L1210 murine leukemias [1].

High impact information on N-(3,4-Dimethyloxyphenethyl)-N-methyl-2-(2-naphthyl)-1,3-dithiane-2-propylamine

Neither Ro-11-2933 nor cyclosporin A, at the maximal tolerated doses in combination with vinblastine, led to significant inhibition of KB-8-5 tumour growth compared to treatment with the two vehicles alone [2].
However, the cytotoxicity of Ro 11-2933 was higher with an IC50 near 20 mumol/I in both K562 and MCF7 cell lines [3].
Similar concentrations of either chlorpromazine or Ro 11-2933/001 lowered the IC50 of the resistant clone to approximately the same level as that observed for the sensitive clone for each of the quinolines tested [4].
The results obtained indicate that RO 11-2933 might represent a promising agent for the reversal of multidrug resistance [1].
In the poorly resistant subline A2780-DX1, a short-term (2 h) exposure to 1 microM RO 11-2933 (IC10) completely restored DX sensitivity, whereas in the more resistant subline A2780-DX3 only partial reversal of drug resistance could be achieved by this schedule of treatment [5].

References

Reversal of doxorubicin and cisplatin resistance in vivo in murine leukemias by the calcium antagonist RO 11-2933. Mazzoni, A., Canti, G. Selective cancer therapeutics. (1990) [Pubmed]
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]
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]
Plasmodium falciparum: modulation by calcium antagonists of resistance to chloroquine, desethylchloroquine, quinine, and quinidine in vitro. Kyle, D.E., Oduola, A.M., Martin, S.K., Milhous, W.K. Trans. R. Soc. Trop. Med. Hyg. (1990) [Pubmed]
In vitro reversal of doxorubicin resistance by the tiapamil analog RO 11-2933 in human ovarian cancer cells. Mazzoni, A. Tumori. (1990) [Pubmed]

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