Recent update on development of small-molecule STAT3 inhibitors for cancer therapy: from phosphorylation inhibition to protein degradation
Signal transducer and activator of transcription 3 (STAT3) is a transcription factor that
regulates various biological processes, including proliferation, metastasis, angiogenesis …
regulates various biological processes, including proliferation, metastasis, angiogenesis …
Medicinal chemistry strategies to discover P-glycoprotein inhibitors: An update
The presence of multidrug resistance (MDR) in malignant tumors is one of the primary
causes of treatment failure in cancer chemotherapy. The overexpression of the ATP binding …
causes of treatment failure in cancer chemotherapy. The overexpression of the ATP binding …
Chalcone: A promising bioactive scaffold in medicinal chemistry
G Rajendran, D Bhanu, B Aruchamy, P Ramani… - Pharmaceuticals, 2022 - mdpi.com
Chalcones are a class of privileged scaffolds with high medicinal significance due to the
presence of an α, β-unsaturated ketone functionality. Numerous functional modifications of …
presence of an α, β-unsaturated ketone functionality. Numerous functional modifications of …
Strategies to overcome cancer multidrug resistance (MDR) through targeting P-glycoprotein (ABCB1): an updated review
The emergence of multidrug resistance (MDR) in malignant tumors is one of the leading
threats encountered currently in many chemotherapeutic agents. The overexpression of the …
threats encountered currently in many chemotherapeutic agents. The overexpression of the …
Discovery of the Triazolo[1,5-a]Pyrimidine-Based Derivative WS-898 as a Highly Efficacious and Orally Bioavailable ABCB1 Inhibitor Capable of Overcoming …
Targeting P-glycoprotein (ABCB1 or P-gp) has been recognized as a promising strategy to
overcome multidrug resistance. Here, we reported our medicinal chemistry efforts that led to …
overcome multidrug resistance. Here, we reported our medicinal chemistry efforts that led to …
Discovery of benzochalcone derivative as a potential antigastric cancer agent targeting signal transducer and activator of transcription 3 (STAT3)
J Dong, J Yang, W Yu, H Li, M Cai, JL Xu… - Journal of Enzyme …, 2022 - Taylor & Francis
Gastric cancer remains a significant health burden worldwide. In continuation of our
previous study and development of effective small molecules against gastric cancer, a series …
previous study and development of effective small molecules against gastric cancer, a series …
Discovery of heterocycle-containing α-naphthoflavone derivatives as water-soluble, highly potent and selective CYP1B1 inhibitors
Abstract Cytochrome P450 1B1 (CYP1B1) has been well validated as an attractive target for
cancer prevention and drug resistance reversal. In continuation of our interest in this area …
cancer prevention and drug resistance reversal. In continuation of our interest in this area …
Synthesis and structure-activity relationship studies of α-naphthoflavone derivatives as CYP1B1 inhibitors
Abstract Cytochrome P450 1B1 (CYP1B1) has been recognized as an important target for
cancer prevention and drug resistance reversal. In order to obtain potent and selective …
cancer prevention and drug resistance reversal. In order to obtain potent and selective …
Excited state intramolecular proton transfer of 2-phenyl, 3-hydroxybenzo [g] quinolones in solution and in G4 supramolecular hydrogels
S Dutta, D Mandal - Journal of Molecular Liquids, 2022 - Elsevier
Abstract The 2-Phenyl, 3-Hydroxybenzo [g] quinolone (2P3HBQ) fluorophore and its
derivative, 2-(4′-hydroxyphenyl)-3-hydroxybenzo [g] quinolone (2HP3HBQ), exhibit well …
derivative, 2-(4′-hydroxyphenyl)-3-hydroxybenzo [g] quinolone (2HP3HBQ), exhibit well …
New perspectives of CYP1B1 inhibitors in the light of molecular studies
R Mikstacka, Z Dutkiewicz - Processes, 2021 - mdpi.com
Human cytochrome P450 1B1 (CYP1B1) is an extrahepatic heme-containing
monooxygenase. CYP1B1 contributes to the oxidative metabolism of xenobiotics, drugs, and …
monooxygenase. CYP1B1 contributes to the oxidative metabolism of xenobiotics, drugs, and …