R17934-NSC 238159: A new antitumor drug—I. Effect on experimental tumors and factors influencing effectiveness

Atassi, Ghanem; Tagnon, Henri

doi:10.1016/0014-2964(75)90092-4

Cited by 31 publications

(19 citation statements)

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“…Nocodazole (methyl [5-(2-thienylcarbonyl)-1Hbenzimidazol-2-yl]) is a synthetic drug that has antimitotic Jordan et al, 1992] and antitumor activities [DeBrabander et al, 1975;Atassi and Tagnon, 1975]. The action of this agent is reversible and rapid .…”

Section: Introductionmentioning

confidence: 99%

Interaction of nocodazole with tubulin isotypes

Schwarz

Ludueña

2002

Drug Development Research

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Nocodazole is an anti-mitotic drug that has long been used as an experimental tool in cell biology. Although nocodazole is known to bind with high affinity to tubulin and to inhibit microtubule assembly, very little has been done on its precise mechanism of action. In fact, its binding to the different isotypes of tubulin has never been addressed. Although the nocodazole binding site overlaps with that of colchicine, the two drugs are structurally quite different. The tubulin molecule is an α/β heterodimer; both α and β exist as various isotypes whose distribution and drug-binding properties are significantly different.In this study, we measured the binding affinity of nocodazole for purified tubulin isotypes. Using fluorescence quenching analysis, we found that the binding kinetics of nocodazole with each type of tubulin best fits a two-affinity Michaelis-Menten binding model. The apparent dissociation constants for the high-affinity binding sites are 0.52 ± 0.02 for αβ II , 1.54 ± 0.29 for αβ III , and 0.29 ± 0.04 for αβ IV . Thus, nocodazole has the highest affinity for αβ IV and the lowest affinity for αβ III . Knowledge of the isotype specificity of nocodazole may allow for development of novel therapeutic agents based on this drug. Drug Dev. Res. 55:91-96, 2002.

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Section: Introductionmentioning

confidence: 99%

Interaction of nocodazole with tubulin isotypes

Schwarz

Ludueña

2002

Drug Development Research

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“…The analytical and spectral data are the tools of the structure elucidation of compound 7. Thus, the 1 H NMR spectrum showed a multiplet at δ1.18 -1.69 ppm indicating the cyclopentene three CH 2 , a singlet at δ2.50 ppm corresponding to the CH 2 group, a singlet at δ4.29 ppm for the thiazol CH 2 , and a singlet at δ8.27 ppm for the NH group (Figure 1).…”

Section: Chemistrymentioning

confidence: 99%

“…Although the number of drugs is available in the market, the need of discovering the new anti-tumor drugs with better pharmacokinetic profile and lesser toxicity has become the main objective in the field of medicinal chemistry, and it is also due to the fast microbial resistance to the existing molecules [1]- [3]. A large number of…”

Section: Introductionmentioning

confidence: 99%

The Synthesis and Cytotoxicity of Novel Thiophene Derivatives Derived from 2-(4-Oxo-4,4-Dihydrothiazol-2-yl) Acetonitrile

Samir¹,

Hamed²

2016

IJOC

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The reaction of the 2-(4-oxo-4,4-dihydrothiazol-2-yl)acetonitrile 1 with cyaclopentanone (2) afforded the condensed product 3. The latter underwent a series of heterocyclizations through its reaction with different reagents. Moreover, compound 1 underwent the Gewald's thiophene to afford compounds 15 and 17. The reaction of either hydrazine hydrate or phenylhydrazine with compound 17 gave the hydrazide derivatives 19a and 19b, respectively. The cytotoxicity of the newly synthesized products was measured towards the three cancer cell lines MCF-7, NCI-H460 and SF-268. The study showed that compounds 3, 5, 9c, 11, 13a, 13c, 17 and 19b were the most active compounds towards the three cancer cell lines.

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“…Cyclophosphamide (NSC-26271) was obtained from the National Cancer Institute, Bethesda, Maryland; Nocodazole (NSC-238159), an experimental antimetastatic drug [3,4], from Janssen Pharmaceutica, Beerse, Belgium; and Adriamycin (NSC-123127), from Farmitalia Benelux. These three drugs were administered i.p.…”

Section: Drugsmentioning

confidence: 99%

“…As indicated in table 5, the simultaneous administration of Nocodazole, a potent antimetastatic [3,4] and anti-invasive [17], and inicarone did not inhibit metastases. When Nocodazole was administered alone, it totally inhibited the appearance of spontaneous metastases.…”

Section: Combination Chemotherapy Of the Fibrinolytic Agent With Chemmentioning

confidence: 99%

Ineffectiveness of inicarone, a fibrinolytic agent, alone or in combination with chemotherapeutic agents on spontaneously metastasizing murine tumours

1983

Self Cite

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The effect of inicarone (L7035), a potent fibrinolytic, alone or in combination, was investigated on spontaneously metastasizing Lewis lung carcinoma (implanted intramuscularly) to verify whether it could prevent the formation of metastases. After intraperitoneal and oral administration, inicarone did not show any cytotoxicity since the survival of animals was not prolonged. Its activity was compared to that of warfarin, an anticoagulant: both drugs were inactive when administered in curative treatment and inicarone even enhanced the number of lung metastases. When administered in combination with cyclophosphamide, an antiproliferative agent, inicarone did not induce any synergism or antagonism, but this combination did not inhibit tumour growth or metastasis spreading. Moreover, when inicarone was combined with a potent antimetastatic agent, Nocodazole, it was shown to be in competition with the latter agent and totally overshadowed its activity; since inicarone had no antimetastatic effect, the number of metastases rose dramatically.

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R17934-NSC 238159: A new antitumor drug—I. Effect on experimental tumors and factors influencing effectiveness

Cited by 31 publications

References 0 publications

Interaction of nocodazole with tubulin isotypes

Interaction of nocodazole with tubulin isotypes

The Synthesis and Cytotoxicity of Novel Thiophene Derivatives Derived from 2-(4-Oxo-4,4-Dihydrothiazol-2-yl) Acetonitrile

Ineffectiveness of inicarone, a fibrinolytic agent, alone or in combination with chemotherapeutic agents on spontaneously metastasizing murine tumours

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