On December 31, 2010, Denora, Nunzio; Laquintana, Valentino; Trapani, Adriana; Lopedota, Angela; Latrofa, Andrea; Gallo, James M.; Trapani, Giuseppe published an article.Quality Control of Methyl 6-chloro-6-oxohexanoate The title of the article was Translocator Protein (TSPO) Ligand-Ara-C (Cytarabine) Conjugates as a Strategy To Deliver Antineoplastic Drugs and To Enhance Drug Clinical Potential. And the article contained the following:
The aim of this work was to evaluate TSPO ligand-Ara-C conjugation as an approach for the selective delivery of the antineoplastic agent to brain tumors as well as for overcome P-gp resistance induction observed for the majority of cytotoxic agents, enhancing the drug clin. potential. To this end, novel N-imidazopyridinacetyl-Ara-C conjugates have been prepared and evaluated for their cytotoxicity against glioma cell lines. Conjugate (I) resulted stable in both phosphate buffer and physiol. medium. In all cases, the release of free Ara-C from hydrolyzed conjugates was checked by HPLC and ESI-MS anal. Conjugates (II) and I displayed very high in vitro TSPO affinity and selectivity, and, hence, they may possess potential for targeted brain delivery. Due to the favorable features displayed by the conjugate I, it was further evaluated on glioma cell lines, expressing high levels of TSPO, in the presence and in the absence of specific nucleoside transport (NT) inhibitors. In contrast to that observed for the free Ara-C, the presence of NT inhibitors did not reduce the cytotoxic activity of I. Moreover, conjugate I, as N4-acyl derivative of Ara-C, should be resistant to inactivation by cytidine deaminase, and it may possess enhanced propensity to target brain tumor cells characterized by a reduced expression of NTs. In addition, this conjugate behaves as a clear P-gp modulator and thereby may be useful to reverse MDR. Transport studies across the MDCKII-MDR1 monolayer indicated that conjugate I should overcome the BBB by transcellular pathway. All these features may be useful for enhancing the clin. potential of the nucleoside drug Ara-C. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Quality Control of Methyl 6-chloro-6-oxohexanoate
The Article related to translocator protein ligand cytarabine conjugate antineoplastic resistance, Pharmaceuticals: Pharmaceutics and other aspects.Quality Control of Methyl 6-chloro-6-oxohexanoate
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