7694-45-3Relevant articles and documents
Novel tdp1 inhibitors based on adamantane connected with monoterpene moieties via heterocyclic fragments
Chepanova, Arina A.,Dyrkheeva, Nadezhda S.,Ilina, Ekaterina S.,Korchagina, Dina V.,Lavrik, Olga I.,Mozhaitsev, Evgenii S.,Munkuev, Aldar A.,Reynisson, Jóhannes,Salakhutdinov, Nariman F.,Suslov, Evgeniy V.,Volcho, Konstantin P.,Zakharenko, Alexandra L.,Zakharova, Olga D.
, (2021/06/12)
Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a promising target for anticancer therapy due to its ability to counter the effects topoisomerase 1 (Top1) poison, such as topotecan, thus, decreasing their efficacy. Compounds containing adamantane and monoterpenoid residues connected via 1,2,4-triazole or 1,3,4-thiadiazole linkers were synthesized and tested against Tdp1. All the derivatives exhibited inhibition at low micromolar or nanomolar concentrations with the most potent inhibitors having IC50 values in the 0.35–0.57 μM range. The cytotoxicity was determined in the HeLa, HCT-116 and SW837 cancer cell lines; moderate CC50 (μM) values were seen from the mid-teens to no effect at 100 μM. Furthermore, citral derivative 20c, α-pinene-derived compounds 20f, 20g and 25c, and the citronellic acid derivative 25b were found to have a sensitizing effect in conjunction with topotecan in the HeLa cervical cancer and colon adenocarcinoma HCT-116 cell lines. The ligands are predicted to bind in the catalytic pocket of Tdp1 and have favorable physicochemical properties for further development as a potential adjunct therapy with Top1 poisons.
Perilla acid methyl ester derivatives containing nitrogen and its preparation and use
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Paragraph 0024; 0025, (2018/04/02)
The invention belongs to the technical field of medicines and relates to a purple perilla methyl rosmarinate nitrogen-containing derivative as well as a preparation method and application thereof, wherein the purple perilla methyl rosmarinate nitrogen-containing derivative has structural characteristics shown in a formula I described in the specification. The invention also relates to pharmaceutically acceptable salt and solvate of the purple perilla methyl rosmarinate nitrogen-containing derivative and a pharmaceutical composition containing the purple perilla methyl rosmarinate nitrogen-containing derivative or pharmaceutically acceptable salt of the purple perilla methyl rosmarinate nitrogen-containing derivative as active ingredients, wherein the pharmaceutically acceptable salt and solvate and the pharmaceutical composition can be used for treating cancer. The purple perilla methyl rosmarinate nitrogen-containing derivative and pharmaceutical salt thereof have good antitumour activities, the preparation method is simple and feasible, and operation is easy.
Oxidative Transformations of Biosourced Alcohols Catalyzed by Earth-Abundant Transition Metals
Nguyen, Duc Hanh,Morin, Yohann,Zhang, Lei,Trivelli, Xavier,Capet, Frédéric,Paul, Sébastien,Desset, Simon,Dumeignil, Franck,Gauvin, Régis M.
, p. 2652 - 2660 (2017/07/28)
The catalytic acceptorless dehydrogenative oxidation of biosourced alcohols into carboxylic acid salts was achieved using earth-abundant Fe and Mn complexes that feature aliphatic PNP pincer ligands in good to excellent yields. The Fe derivatives were characterized by using 57Fe NMR spectroscopy. Mn pincer catalysts are catalytically more efficient than their Fe counterparts thanks to their robustness under basic conditions. Attempts to generate aldehydes from alcohols were not successful using the Fe and Mn species, but a commercially available Ru analogue achieves this transformation selectively under very mild conditions in the presence of a large excess of acetone as a hydrogen acceptor.
