An article New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors WOS:000496249500080 published article about DNA PHOSPHODIESTERASE 1; EMPIRICAL SCORING FUNCTIONS; PROTEIN-LIGAND DOCKING; BIOLOGICAL EVALUATION; IN-VITRO; THIOSEMICARBAZONES; TOPOISOMERASES; IDENTIFICATION; ANTICANCER; COMPLEXES in [Filimonov, Aleksander S.; Luzina, Olga A.; Volcho, Konstantin P.; Salakhutdinov, Nariman F.; Lavrik, Olga, I] Russian Acad Sci, NN Vorozhtsov Novosibirsk Inst Organ Chem, Siberian Branch, 9 Akad Lavrentieva Ave, Novosibirsk 630090, Russia; [Chepanova, Arina A.; Zakharenko, Alexandra L.; Zakharova, Olga D.; Ilina, Ekaterina S.; Dyrkheeva, Nadezhda S.; Kuprushkin, Maxim S.] Russian Acad Sci, Novosibirsk Inst Chem Biol & Fundamental Med, Siberian Branch, 8 Akad Lavrentieva Ave, Novosibirsk 630090, Russia; [Filimonov, Aleksander S.; Volcho, Konstantin P.; Salakhutdinov, Nariman F.; Lavrik, Olga, I] Novosibirsk State Univ, Pirogova Str 1, Novosibirsk 630090, Russia; [Kolotaev, Anton, V; Khachatryan, Derenik S.] Natl Res Ctr, Fed State Unitary Enterprise, Inst Chem Reagents & High Pur Chem Subst, Kurchatov Inst, Moscow 107076, Russia; [Patel, Jinal; Leung, Ivanhoe K. H.; Chand, Raina; Ayine-Tora, Daniel M.] Univ Auckland, Sch Chem Sci, Auckland 1142, New Zealand; [Reynisson, Johannes] Keele Univ, Sch Pharm & Bioengn, Hornbeam Bldg, Keele ST5 5BG, Staffs, England in 2019.0, Cited 61.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Recommanded Product: 500-22-1
Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a promising therapeutic target in cancer therapy. Combination chemotherapy using Tdp1 inhibitors as a component can potentially improve therapeutic response to many chemotherapeutic regimes. A new set of usnic acid derivatives with hydrazonothiazole pharmacophore moieties were synthesized and evaluated as Tdp1 inhibitors. Most of these compounds were found to be potent inhibitors with IC50 values in the low nanomolar range. The activity of the compounds was verified by binding experiments and supported by molecular modeling. The ability of the most effective inhibitors, used at non-toxic concentrations, to sensitize tumors to the anticancer drug topotecan was also demonstrated. The order of administration of the inhibitor and topotecan on their synergistic effect was studied, suggesting that prior or simultaneous introduction of the inhibitor with topotecan is the most effective.
About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Filimonov, AS; Chepanova, AA; Luzina, OA; Zakharenko, AL; Zakharova, OD; Ilina, ES; Dyrkheeva, NS; Kuprushkin, MS; Kolotaev, AV; Khachatryan, DS; Patel, J; Leung, IKH; Chand, R; Ayine-Tora, DM; Reynisson, J; Volcho, KP; Salakhutdinov, NF; Lavrik, OI or concate me.. Recommanded Product: 500-22-1
Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem