- Synthesis and anticancer evaluation of vitamin K3 analogues
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Novel vitamin K3 analogues were synthesized and evaluated for their anticancer activity. Compound 6, 9, 10, 11, 14, and (±)15 demonstrated a strong inhibitory activity against the tumor cells of A-549, Hep G2, MCF7, MES-SA, MES-SA/Dx5, MKN45, S
- Chen, Chinpiao,Liu, Yi-Zhong,Shia, Kak-Shan,Tseng, Huan-Yi
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- The role of a quinone methide in the sequence specific alkylation of DNA
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Oligonucleotide-naphthoquinone conjugates were prepared and examined for use as inducible, site-directed alkylating agents of DNA. Reaction was found to be sequence specific and under control of either biomimetic reduction or near-UV irradiation. Both conditions induced the formation of a transient and highly electrophilic intermediate consistent with a quinone methide. Enzymatic reduction of 5-((mesyloxy)methyl)- and 5-(bromomethyl)naphthoquinone derivatives produced cross-linking between a target and probe sequence, but the equivalent 5-(acetoxymethyl), 5-(hydroxymethyl) and 5-methyl analogues were predictably inactive. Conversely, irradiation of the 5-methylnaphthoquinone derivative produced cross-linking through a mechanism of photochemical enolization that was not available to the 6-methyl, 3-methyl, or unsubstituted analogues. Hydroxyl radical footprinting of the modified DNA demonstrated that guanine and cytosine were targets of alkylation.
- Chatterjee, Moneesh,Rokita, Steven E.
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- THERAPEUTIC COMPOUNDS AND METHODS
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The invention relates to compounds of Formula (I) and methods for their preparation. Also described are pharmaceutical compositions comprising a compound of Formula (I) and their use in the treatment or prevention of conditions associated with mitochondrial dysfunction. Formula (I)
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Page/Page column 0177
(2018/11/22)
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- Exploring synthetic avenues for the effective synthesis of selenium- and tellurium-containing multifunctional redox agents
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Various human illnesses, including several types of cancer and infectious diseases, are related to changes in the cellular redox homeostasis. During the last decade, several approaches have been explored which employ such disturbed redox balances for the
- Mecklenburg, Susanne,Shaaban, Saad,Ba, Lalla A.,Burkholz, Torsten,Schneider, Thomas,Diesel, Britta,Kiemer, Alexandra K.,Roeseler, Anne,Becker, Katja,Reichrath, Joerg,Stark, Alexandra,Tilgen, Wolfgang,Abbas, Muhammad,Wessjohann, Ludger A.,Sasse, Florenz,Jacob, Claus
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scheme or table
p. 4753 - 4762
(2009/12/08)
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- Novel naphthoquinone and quinolinedione inhibitors of CDC25 phosphatase activity with antiproliferative properties
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CDC25 phosphatases are considered as attractive targets for anti-cancer therapy. To date, quinone derivatives are among the most potent inhibitors of CDC25 phosphatase activity. We present in this paper the synthesis and the biological evaluation of new q
- Braud, Emmanuelle,Goddard, Mary-Lorene,Kolb, Stephanie,Brun, Marie-Priscille,Mondesert, Odile,Quaranta, Muriel,Gresh, Nohad,Ducommun, Bernard,Garbay, Christiane
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scheme or table
p. 9040 - 9049
(2009/04/11)
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