Authors Silbermann, K; Shah, CP; Sahu, NU; Juvale, K; Stefan, SM; Kharkar, PS; Wiese, M in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about RESISTANCE-ASSOCIATED PROTEIN-1; MEDIATED MULTIDRUG-RESISTANCE; TYROSINE KINASE INHIBITORS; G MEMBER 2; P-GLYCOPROTEIN; BIOLOGICAL EVALUATION; DRUG-RESISTANCE; IN-VITRO; PYRROLOPYRIMIDINE DERIVATIVES; HIGHLY POTENT in [Shah, Chetan P.; Sahu, Niteshkumar U.; Juvale, Kapil; Kharkar, Prashant S.] SVKMs NMIMS, Shobhaben Pratapbhai Patel Sch Pharm & Technol Ma, VL Mehta Rd, Mumbai 400056, India; [Silbermann, Katja; Stefan, Sven Marcel; Wiese, Michael] Rheinische Friedrich Wilhelms Univ Bonn, Inst Pharmaceut, Pharmaceut Chem 2, Immenburg 4, D-53121 Bonn, Germany in 2019.0, Cited 65.0. SDS of cas: 99-93-4. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4
During cancer chemotherapy, certain cancers may become cross-resistant to structurally diverse antineoplastic agents. This so-called multidrug resistance (MDR) is highly associated with the overexpression of ATP-binding cassette (ABC) transport proteins. These membrane-bound efflux pumps export a broad range of structurally diverse endo- and xenobiotics, including chemically unrelated anticancer agents. This translocation of drugs from the inside to the outside of cancer cells is mediated at the expense of ATP. In the last 40 years, three ABC transporters – ABCB1 (P-gp), ABCC1 (MRP1), and ABCG2 (BCRP) – have mainly been attributed to the occurrence of MDR in cancer cells. One of the strategies to overcome MDR is to inhibit the efflux transporter function by small-molecule inhibitors. In this work, we investigated new chalcone- and flavone-based compounds for selective as well as broad-spectrum inhibition of the stated transport proteins. These include substituted chalcones with variations at rings A and B, and flavones with acetamido linker at position 3. The synthesized molecules were evaluated for their inhibitory potential against ABCB1, ABCC1, and ABCG2 in calcein AM and pheophorbide A assays. In further investigations with the most promising candidates from each class, we proved that ABCB1- and ABCG2-mediated MDR could be reversed by the compounds. Moreover, their intrinsic toxicity was found to be negligible in most cases. Altogether, our findings contribute to the understanding of ABC transport proteins and reveal new compounds for ongoing evaluation in the field of ABC transporter-mediated MDR. (C) 2018 Elsevier Masson SAS. All rights reserved.
SDS of cas: 99-93-4. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Silbermann, K; Shah, CP; Sahu, NU; Juvale, K; Stefan, SM; Kharkar, PS; Wiese, M or concate me.
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,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles