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Vinca vinflunine

Ngan VK, Bellman K, Hill BT et al (2001) Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine. Mol Pharmacol 60 225-232... [Pg.417]

Vinblastine (105) Vinca alkaloid Vinflunine (Javlor ) Oncology Tubulin binding Phase III Pierre Fabre 682-687... [Pg.68]

Vinca dimer indole alkaloids (e.g. vinbiastine) act as spindle poisons. They bind tubulin, inhibiting polymerisation into microtubules, the major elements of the cytoskeleton [100]. Vinblastine itself and its analogue vinoreibine (Navelbine ) [101] are marketed for cancer therapies (Fig. 36). Vinflunine (Javlor ) is a member of second-generation Vinca dimer alkaloids. This 4 -difluoro analogue is more active than vinoreibine in several cancers (Fig. 36). It is now in phase III clinical... [Pg.585]

An MAA for vinflunine (Javlor ) 43 (Pierre Fabre) has been submitted to the European Medicines Agency (EMEA) for the treatment of various cancers.103 Pierre Fabre had been developing vinflunine 43104 106 in the USA in partnership with Bristol-Myers Squibb for the treatment of breast, bladder and lung cancers but development was halted in late 2007.107 Four Vinca-type alkaloids have been approved for cancer treatment vinblastine 44108 and vincristine... [Pg.332]

Kruczynski A, Barret JM, Erievant C, Colpaert F, Fahy J, Hill BT. Antimitotic and tubulin-interacting properties of vinflunine, a novel fluorinated Vinca alkaloid. Biochem. Pharmacol. 1998 55 635-648. [Pg.1193]

A nice example of using an allometric approach combined with a population data analysis has been prospectively implemented for vinflunine, a third generation of semisynthetic vinca alkaloids, which is an analog of vinorelbine. The authors took... [Pg.793]

Vinblastine and vincristine have been used clinically for many years. The major importance of vinblastine is as part of a combination treatment for Hodgkin s disease, while vincristine is used in combination chemotherapy of acute lymphoblastic leukemias and lymphomas. Several analogues of the vinca alkaloids have entered clinical use or clinical trials, including vindesine (3), vinorelbine (4), " the naturally occurring anhydrovin-blastine (5), and vinflunine (6). ° Several synthetic approaches to the vinca alkaloids have been developed, especially by Kuehne, while studies of the chemistry of the alkaloids in super acidic media have yielded new alkaloids such as vinflunine. ... [Pg.7]

The vinflunine case demonstrated that the Vinca alkaloids remain a drug family where it is still possible to identify new members with unprecedented and promising pharmacological properties. When the ongoing research on the mechanisms of action of Vinca alkaloids unravels the precise relation structure/function of the dimeric molecules, it should be possible to rationally design a new generation of Vinca alkaloids with new therapeutic properties. [Pg.819]

Vindoline and catharanthine are the last monomeric precursors of the dimeric anticancer alkaloids of C. roseus, and they are also the two major alkaloids accumulated in the leaves of the plant [106, 107], The study of the dimerization biosynthetic step stems in early work on the chemical synthesis of the dimeric alkaloids and it has involved much discussion. Moreover, the chemical dimerization reaction has industrial application in the synthesis of vinorelbine and vinflunine. Due to its potential regulatory importance for the production of the dimeric Vinca alkaloids in the plant, and to the much that is known about the chemical and biosynthetic reactions, the dimerization step will be presented in particular detail here. [Pg.827]

The modified Polonovski reaction first used in [19] and later called the Potier-Polonovski reaction, resulted in the formation of an iminium dimer which, after reduction with NaBELt, yielded a-3 ,4 -anhydrovinblastine, Fig. (2). Thus, this was the first dimeric Vinca alkaloid with the natural configuration to be synthesized. This method allowed, subsequently, the development of approaches to the synthesis of other natural dimerics like vinblastine, vincristine, leurosidine and leurosine [110-114], and more recently, to the semisynthetic vinorelbine and vinflunine [16, 22]. [Pg.828]

An effect of Vinca alkaloids that may also be important in their anti tumour activity is their antivascular action. It has been shown that vincristine and vindesine are able to reduce the capillaiy network formation by HUVEC cells cultured on Matrigel at non-cytotoxic concentrations, while vinblastine and vinorelbine produce anti-angiogenic effects by direct cytotoxicity [185]. Vinflunine seems to have an antivascular activity consistently superior to that of vinorelbine [25]. [Pg.841]

When incubated with human hepatocytes, vinorelbine was the most rapidly and intensely accumulated Vinca alkaloid followed by vinblastine, vindesine and vincristine, as would be suggested by the lipophilicities of the molecules [187]. Vinflunine is even more lipophilic than vinorelbine and accumulates taster inside cells [23]. [Pg.842]

The compounds resulting from metabolism of the Vinca alkaloids are little characterized. The main hepatic metabolite of vinblastine, vincristine, vinorelbine and vinflunine seems to be, for each of the compounds, the respective 4-0-deacetyl alkaloid. Other metabolites have also been detected but only very seldom were structurally characterized [15, 191, 200-203],... [Pg.844]


See other pages where Vinca vinflunine is mentioned: [Pg.416]    [Pg.586]    [Pg.617]    [Pg.333]    [Pg.25]    [Pg.416]    [Pg.1112]    [Pg.1143]    [Pg.3632]    [Pg.496]    [Pg.735]    [Pg.814]    [Pg.819]    [Pg.838]    [Pg.838]    [Pg.839]    [Pg.840]    [Pg.842]    [Pg.1465]    [Pg.4334]   
See also in sourсe #XX -- [ Pg.29 ]




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