769968-17-4Relevant academic research and scientific papers
Regioselective 15-bromination and functionalization of a stable synthetic bacteriochlorin
Fan, Dazhong,Taniguchi, Masahiko,Lindsey, Jonathan S.
, p. 5350 - 5357 (2007)
(Chemical Equation Presented) 5-Methoxy-8,8,18,18-tetramethyl-2,12-di-p- tolylbacteriochlorin (MeO-BC) undergoes regioselective electrophilic bromination with NBS to give the 15-bromo analogue (MeO-BC-Br15) in 85% yield. By contrast, the bacter
Synthesis and evaluation of bifunctional PTP4A3 phosphatase inhibitors activating the ER stress pathway
Rastelli, Ettore J.,Sannino, Sara,Hart, Duncan J.,Sharlow, Elizabeth R.,Lazo, John S.,Brodsky, Jeffrey L.,Wipf, Peter
supporting information, (2021/06/21)
We developed JMS-053, a potent inhibitor of the dual specificity phosphatase PTP4A3 that is potentially suitable for cancer therapy. Due to the emerging role of the unfolded protein response (UPR) in cancer pathology, we sought to identify derivatives that combine PTP4A3 inhibition with induction of endoplasmatic reticulum (ER) stress, with the goal to generate more potent anticancer agents. We have now generated bifunctional analogs that link the JMS-053 pharmacophore to an adamantyl moiety and act in concert with the phosphatase inhibitor to induce ER stress and cell death. The most potent compound in this series, 7a, demonstrated a ca. 5-fold increase in cytotoxicity in a breast cancer cell line and strong activation of UPR and ER stress response genes in spite of a ca. 13-fold decrease in PTP4A3 inhibition. These results demonstrate that the combination of phosphatase inhibition with UPR/ER-stress upregulation potentiates efficacy.
GPR35 MODULATORS
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, (2020/08/13)
Described herein are GPR35 modulators and methods of using these compounds in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
AMIDE COMPOUND HAVING BET PROTEOLYSIS-INDUCING ACTION AND MEDICINAL APPLICATION THEREOF
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Paragraph 0267-0269, (2020/01/31)
The present invention aims to provide a compound that: has an excellent cytotoxic action on cancer cells, excellent induction of BET protein degradation in cancer cells, and an excellent binding-inhibiting action on BET protein and acetylated histone; and is effective as an anti-cancer agent, a BET protein degradation-inducing agent, or a BET protein inhibiting agent. A compound indicated in general formula (I) or a pharmacologically acceptable salt thereof. {In the formula, each symbol is as outlined in the Description.}
A trifluorinated thiazoline scaffold leading to pro-apoptotic agents targeting prohibitins
Pérez-Perarnau, Alba,Preciado, Sara,Palmeri, Claudia Mariela,Moncunill-Massaguer, Cristina,Iglesias-Serret, Daniel,González-Gironès, Diana M.,Miguel, Miriam,Karasawa, Satoki,Sakamoto, Satoshi,Cosialls, Ana M.,Rubio-Pati?o, Camila,Saura-Esteller, José,Ram?n, Rosario,Caja, Laia,Fabregat, Isabel,Pons, Gabriel,Handa, Hiroshi,Albericio, Fernando,Gil, Joan,Lavilla, Rodolfo
supporting information, p. 10150 - 10154 (2015/03/31)
A new class of small molecules, with an unprecedented trifluorothiazoline scaffold, were synthesized and their pro-apoptotic activity was evaluated. With an EC50 in the low micromolar range, these compounds proved to be potent inducers of apopt
ANTIVIRAL COMPOUNDS
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Page/Page column 434; 435, (2014/09/29)
The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
