Synthesis and biotesting of new carrier prodrugs of 2-methoxyestradiol

Lozinskaya, N. A.; Maximova, Natalia A.; Bazanov, Daniil R.; Sosonyuk, S. E.; Wobith, Birgit; Зефиров, Н. С.; Kharitonashvili, E.V.; Zefirova, O. N.; Kuznetsov, Sergey A.; Проскурнина, М. В.

doi:10.1016/j.mencom.2020.01.002

Cited by 3 publications

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“…Above problems can be solved by switching salt structures of DCA to covalent derivatives of dichloroacetic acid, capable of releasing the dichloroacetate anion during metabolism, for example, esters [8]. Thus, optimization of the conditions for the synthesis of polyfunctional derivatives of dichloroacetic acid is an important problem in the synthesis of dichloroacetate prodrugs.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Covalent Conjugates of Dichloroacetic Acid with Polyfunctional Compounds

et al. 2021

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The development of prodrugs with an ester bond is classical tool to enhance the bioavailability of pharmaceutical compounds including readily ionizable molecules, such as acids or phenols. In this work, we studied the introduction of a dichloroacetic acid fragment into a molecule as an approach to anticancer prodrug development. The metabolically released dichloroacetate will have an additional useful effect by altering the respiratory cycle of cancer cells and promoting their apoptosis. Derivatives of vitamins B1 and C, paracetamol, and salicylic acid, often used in concomitant cancer therapy, were prepared, and the possibility of selective modifi cation of other polyfunctional compounds was studied. The difference in the reactivity of hydroxy groups in tris(hydroxyphenyl)-substituted cis-imidazoline was studied.

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Section: Introductionmentioning

confidence: 99%