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Chemical Compound Review

Tubulozole     ethylN-[4-[[2-(2,4- dichlorophenyl)-2...

Synonyms: SureCN11113473, NSC-376450, AC1L1KPZ, NSC376450, 84697-22-3, ...
 
 
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Disease relevance of NSC376450

 

High impact information on NSC376450

  • Effects of tubulozole on the microtubule system of cells in culture and in vivo [2].
  • Inhibitors of protein biosynthesis, however, did not show synergistic activity with tubulozole [3].
  • 2. Functional studies demonstrated that vincristine, tubulozole, podophyllotoxin, and demecolcine inhibited nAChR-stimulated catecholamine release noncompetitively and in a concentration-dependent manner, with IC50 values of 3 (1-10), 5 (2-10), 8 (4-15), and 19 (9-39) microM, respectively [4].
  • We have used the synthetic microtubule inhibitor Tubulozole C in order to study the role of the microtubule system in human lymphocyte activation [5].
  • For the cis and trans stereoisomers of the synthetic anti-microtubule compound tubulozole, at micromolar concentrations, tubulozole-C is cytotoxic to mammalian cells whereas tubulozole-T is not [6].
 

Biological context of NSC376450

 

Anatomical context of NSC376450

 

Associations of NSC376450 with other chemical compounds

  • Erbulozole (R55 104) is a water soluble congener of the microtubule inhibitor tubulozole, which has proven to possess anti-invasive, antitumoral and radiosensitizing capacities [11].
 

Gene context of NSC376450

  • Since tubulozole C prevents polymerization of mammalian tubulin whereas tubulozole T does not, the antimalarial action of tubulozoles may not involve microtubules [12].
  • The Kidney Invasion Test: an assay allowing macroscopic quantification of malignant invasion in vivo. Comparison between the microtubule inhibitor tubulozole and the podophyllotoxin congener etoposide (VP-16-213) [13].
 

Analytical, diagnostic and therapeutic context of NSC376450

  • The interactive effect is maintained in a clinically relevant dose fractionation schedule whereby 8 fractions of 2 Gy each were pretreated 6 hr before with 80 mg/kg tubulozole [1].
  • Analysis of labelled parasite proteins by two-dimensional gel electrophoresis showed that while it inhibited synthesis of most proteins to the same degree, tubulozole T super-inhibited the synthesis of certain proteins [12].
  • Eighty mg/kg R 55 104, given orally 6 h before or 3 h after radiotherapy, displays a prominent interactive effect with 10 Gy gamma irradiation in subcutaneous murine tumors which is similar to 160 mg/kg tubulozole administered 6 h before 10 Gy [14].

References

  1. Interaction between the microtubule inhibitor tubulozole and gamma-irradiation in murine tumors in vivo. Distelmans, W., Van Ginckel, R., Vanherck, W., Willebrords, R., De Brabander, M., Wouters, L., Van den Winkel, P., De Backer, G. Int. J. Radiat. Oncol. Biol. Phys. (1989) [Pubmed]
  2. Effects of tubulozole on the microtubule system of cells in culture and in vivo. Geuens, G.M., Nuydens, R.M., Willebrords, R.E., Van de Veire, R.M., Goossens, F., Dragonetti, C.H., Mareel, M.M., De Brabander, M.J. Cancer Res. (1985) [Pubmed]
  3. Mode of action of tubulozoles against Plasmodium falciparum in vitro. Dieckmann-Schuppert, A., Franklin, R.M. Antimicrob. Agents Chemother. (1990) [Pubmed]
  4. Effects of antimitotic agents on secretion and detergent extractibility of adrenal nicotinic acetylcholine receptors. Lopez, I., McKay, D.B. Cell. Mol. Neurobiol. (1997) [Pubmed]
  5. A cytoskeleton-dependent pathway for induction of IL-2 production and a cytoskeleton-independent pathway for IL-2-mediated signal transduction. Nihlmark, E.L., Lindqvist, C. Cell. Immunol. (1989) [Pubmed]
  6. Effect of the anti-microtubule compound tubulozole on Leishmania protozoan parasites in vitro. Fong, D. FEMS Microbiol. Lett. (1993) [Pubmed]
  7. Effect of tubulozole, a new synthetic microtubule inhibitor, on the induction of casein gene expression by prolactin. Servely, J.L., Geuens, G.M., Martel, P., Houdebine, L.M., de Brabander, M. Biol. Cell (1987) [Pubmed]
  8. New structural analogues of Tubulozole induce apoptosis, [Ca2+]i modifications and cytoskeletal disorganization in glial (GL15) and neuronal-like (PC12) cell lines. Castellano, S., Mariggiò, M.A., Guarnieri, S., Stefancich, G., Pietrangelo, T. Arch. Pharm. (Weinheim) (2000) [Pubmed]
  9. Effects of tubulozole on the amoeboflagellate transformation in Physarum polycephalum. Adelman, M.R. Cell Biol. Int. Rep. (1992) [Pubmed]
  10. Comparison of the effects of antimitotic drugs on alpha-tubulin mRNA, microtubules and nicotinic receptor-mediated catecholamine secretion in adrenal chromaffin cells in culture. Gu, H., McKay, S.B., Burkman, A.M., McKay, D.B. Gen. Pharmacol. (1994) [Pubmed]
  11. Phase I trial of erbulozole (R55104). Van Belle, S.J., Distelmans, W., Vandebroek, J., Bruynseels, J., Van Ginckel, R., Storme, G.A. Anticancer Res. (1993) [Pubmed]
  12. Effects of microtubule inhibitors on protein synthesis in Plasmodium falciparum. Bell, A., Wernli, B., Franklin, R.M. Parasitol. Res. (1993) [Pubmed]
  13. The Kidney Invasion Test: an assay allowing macroscopic quantification of malignant invasion in vivo. Comparison between the microtubule inhibitor tubulozole and the podophyllotoxin congener etoposide (VP-16-213). Distelmans, W., Van Ginckel, R., Vanherck, W., De Brabander, M. Invasion Metastasis (1985) [Pubmed]
  14. Influence of the synthetic microtubule inhibitor erbulozole (P.I.N.N.) (R 55 104), a new tubulozole congener, and gamma irradiation on murine tumors in vivo. Distelmans, W., Van Ginckel, R., Vanherck, W., Willebrords, R., De Brabander, M., Wouters, L., Heeres, J. European journal of cancer & clinical oncology. (1989) [Pubmed]
 
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