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; Ginckel, R. Van; Vanherck, W.; Willebrords, R.; Brrabander, M. De; Wouters, Luc; Heeres, Jan

doi:10.1016/0277-5379(89)90111-9

Cited by 3 publications

(1 citation statement)

References 5 publications

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“…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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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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Molecular and cellular basis of cancer invasion and metastasis: Implications for treatment

Jiang

Puntis

Hallett

1994

Journal of British Surgery

120

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In the past decade significant advances in establishing the underlying biological mechanisms of tumour invasion and metastasis have been made. Some of the triggering factors and genes relevant to metastatic spread have been identified. Advances have also been made in understanding the signal transduction pathways involved in invasion and metastasis. This increased comprehension of the malignant metastatic process has enabled new antimetastatic strategies to be devised. This review summarizes progress in these areas and discusses the implications for the treatment of metastasis.

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Spermatogenesis inFasciola hepatica:an ultrastructural comparison of the effects of the anthelmintic, thiabendazole (“Fasinex”) and the microtubule inhibitor, tubulozole

Stitt

Fairweather²

1992

Invertebrate Reproduction & Development

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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

Cited by 3 publications

References 5 publications

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, [Ca2+]i Modifications and Cytoskeletal Disorganization in Glial (GL15) and Neuronal-like (PC12) Cell Lines

Molecular and cellular basis of cancer invasion and metastasis: Implications for treatment

Spermatogenesis inFasciola hepatica:an ultrastructural comparison of the effects of the anthelmintic, thiabendazole (“Fasinex”) and the microtubule inhibitor, tubulozole

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