The effects of tubulazole, a new synthetic microtubule inhibitor on experimental neoplasms

Ginckel, R. Van; Brabander, M. De; Vanherck, W.; Heeres, Jan

doi:10.1016/0277-5379(84)90040-3

Cited by 20 publications

(6 citation statements)

References 3 publications

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“…Tubulozole-C, but not tubulozole-T, inhibits mammalian cells in culture, and is also active against tumors in vivo [13,17]. For epithelial cell lines, such as mouse embryonic MO 4 cells and rat kangaroo PTK 2 cells, the microtubules and subcellular organelles are apparently normal for cells treated with tubulozole-T up to 18 /zM for 24 h [13].…”

Section: Discussionmentioning

confidence: 99%

Effect of the anti-microtubule compound tubulozole on Leishmania protozoan parasites in vitro

Fong

1993

FEMS Microbiology Letters

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For the c/s 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. The effect of tubulozoles on the parasitic protozoan Leishmania was tested. For the promastigote stage of L. mexicana amazonensis, both isomers inhibited parasite growth. For the amastigote stage of L. mexicana amazonensis and L. major, within murine J774 macrophage line as host cells in vitro, tubulozole-T reduced the infective index. Despite the observation of macrophage cytotoxicity of tubulozole-T, this compound may be a potentially useful and novel anti-leishmanial drug.

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Section: Discussionmentioning

confidence: 99%

Effect of the anti-microtubule compound tubulozole on Leishmania protozoan parasites in vitro

Fong

1993

FEMS Microbiology Letters

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“…Presumably, this is the cause of its antitumoral effect [1,2,20] . Furthermore, it has been shown that the microtubule disruption can lead to apoptosis [21,22,23] .…”

Section: As Reported Inmentioning

confidence: 99%

“…Tubulozole has been extensively studied in different tumour models: all trials have shown a prolonged median survival time in mice and distinct antineoplastic properties. All the in vivo as well in vitro activity of Tubulozole resides exclusively in the cis isomer [2] . In addition, Erbulozole, the structural analogue of Tubulozole in which the 2,4-dichlorobenzene moiety is replaced by the 4-methoxybenzene unit (Figure 1), exhibits an antimicrotubular effect on cell cultures at doses tenfold lower than those of the parent compound [3,4] .…”

Section: Introductionmentioning

confidence: 99%

New Structural Analogues of Tubulozole Induce Apoptosis, [Ca2+]i Modifications and Cytoskeletal Disorganization in Glial (GL15) and Neuronal-like (PC12) Cell Lines

Castellano

Mariggiò

Guarnieri

et al. 2000

Arch. Pharm. Pharm. Med. Chem.

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The synthesis and the biological activity of (±)‐cis‐ and (±)‐trans‐[4‐[[2‐(1,1´‐biphenyl‐4‐yl)‐2‐(1H‐imidazol‐1‐ylmethyl)‐1,3‐dioxolan‐4‐yl]methylthio]phenyl]carbamic acid ethyl esters (2a and 2b) are discussed. They were designed as structural analogues of Tubulozole, a synthetic tubulin polymerisation inhibitor with antimitotic properties. Biological tests were carried out on PC12, a neuronal‐like cell line derived from rat pheochromocytoma, and on GL15, a cell line derived from human glioblastoma. The exposure (from 5 to 20 h) of GL15 and PC12 cells to different concentrations (0.1—1000 μM; IC50 ~1 μM) of 2a or 2b resulted in a drastic decrease in the number of viable cells without an apparent effect on the cell distribution in the various phases of the cell cycle. Compound 2a or 2b (10 μM) induced cell death by activating apoptosis. This was correlated with the activation of an oscillating Ca 2+‐dependent mechanism which increased the intracellular calcium concentration ([Ca 2+]i) via Ca 2+‐release from internal stores. Moreover, 2a (10 μM) also induced severe damage of cytoskeletal F‐actin filaments after a 5 h incubation in GL15 cells. This was also observed but to a smaller extent, for 2b. Under the same experimental conditions, PC12 cells showed similar actin deregulation.

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“…Tubulozole is capable of interfering with the cytoskeletal organisation by interaction with tubulin or some other component of the microtubules. Presumably, this is the cause of its antitumoral effect [1,2,20] . Furthermore, it has been shown that the microtubule disruption can lead to apoptosis [21,22,23] .…”

Section: As Reported Inmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

New Structural Analogues of Tubulozole Induce Apoptosis, [Ca 2+]i Modifications and Cytoskeletal Disorganization in Glial (GL15) and Neuronal-like (PC12) Cell Lines

Castellano¹,

Mariggiò²,

Guarnieri³

et al. 2000

Arch. Pharm. Pharm. Med. Chem.

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The effects of tubulazole, a new synthetic microtubule inhibitor on experimental neoplasms

Cited by 20 publications

References 3 publications

Effect of the anti-microtubule compound tubulozole on Leishmania protozoan parasites in vitro

Effect of the anti-microtubule compound tubulozole on Leishmania protozoan parasites in vitro

New Structural Analogues of Tubulozole Induce Apoptosis, [Ca2+]i Modifications and Cytoskeletal Disorganization in Glial (GL15) and Neuronal-like (PC12) Cell Lines

New Structural Analogues of Tubulozole Induce Apoptosis, [Ca 2+]i Modifications and Cytoskeletal Disorganization in Glial (GL15) and Neuronal-like (PC12) Cell Lines

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