25026-34-0Relevant articles and documents
Synthesis and in vitro platelet aggregation and TP receptor binding studies on bicyclic 5,8-ethanooctahydroisoquinolines and 5,8-ethanotetrahydroisoquinolines
Saha, Shankar L,Roche, Victoria F,Pendola, Kathleen,Kearley, Mark,Lei, Longping,Romstedt, Karl J,Herdman, Mark,Shams, Gamal,Kaisare, Vivek,Feller, Dennis R
, p. 2779 - 2793 (2002)
Eighteen novel bicyclic 1-substituted benzyl octahydro- and tetrahydroisoquinolines were synthesized and evaluated for human thromboxane A2/prostaglandin H2 (TP) receptor affinity and antagonism of TP receptor-mediated platelet aggre
Design, Synthesis, and Biological Evaluation of Pyrazole Derivatives
Hu, Chunqi,Gao, Yali,Du, Wenting
, p. 673 - 679 (2016)
In this in vitro study, a series of novel pyrazole derivatives were designed, synthesized, and evaluated against five human cancer cell lines (PC3, A549, HL60, HCT116, and SW620) for their antiproliferative and p53-MDM2 binding inhibitory activities. Although biological evaluations showed that this series of compounds possessed weak p53-MDM2 inhibitory activities, most of them displayed moderate to potent antiproliferative activities against the tested cells lines. Compound 11c exhibited the best potency for MDM2 (FP-IC50 = 29.22 μm) and demonstrated antiproliferative activities in response to the five tested cell lines (IC50 = 4.09-16.82 μm). Compared with the positive control Nutlin-1, there was enhanced antiproliferative activity to p53-mutated or p53-deficient cell lines (SW620, HL60, and PC3).
Synthesis, Characterization and Antimicrobial Activity of N-2-(4-Chlorophenyl)acetyl Derivatives of (S)-Amino Acids
Venkateshappa,Raghavendra Kumar,Krishna
, p. 381 - 384 (2020/01/08)
This paper reports the synthesis, characterization and antibacterial activity of N-2-(4-chlorophenyl)acetyl derivatives of various (S)-amino acids such as (S)-alanine, (S)-phenylalanine, (S)-leucine, (S)-methionine, (S)-proline and (S)-tryptophane. These
Preparation of Organic Nitrates from Aryldiazoacetates and Fe(NO3)3·9H2O
Thurow, Samuel,Fernandes, Alessandra A. G.,Quevedo-Acosta, Yovanny,De Oliveira, Matheus F.,De Oliveira, Marcelo G.,Jurberg, Igor D.
supporting information, p. 6909 - 6913 (2019/09/12)
A thermal protocol is reported for the formal insertion of nitric acid into aryldiazoacetates using Fe(NO3)3·9H2O. This strategy is mild and high yielding and allows the preparation of a large variety of members of an unprecedented family of organic nitrates. The nitrate group can be also readily transformed into other functional groups and heterocyclic moieties and can possibly allow new biological explorations of untapped potential associated with their NO-releasing ability.
Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors Showing Partial Cross-Resistance with Quinolones
Jeannot, Frédéric,Taillier, Thomas,Despeyroux, Pierre,Renard, Stéphane,Rey, Astrid,Mourez, Micha?l,Poeverlein, Christoph,Khichane, Imène,Perrin, Marc-Antoine,Versluys, Stéphanie,Stavenger, Robert A.,Huang, Jianzhong,Germe, Thomas,Maxwell, Anthony,Cao, Sha,Huseby, Douglas L.,Hughes, Diarmaid,Bacqué, Eric
, p. 3565 - 3581 (2018/05/01)
In our quest for new antibiotics able to address the growing threat of multidrug resistant infections caused by Gram-negative bacteria, we have investigated an unprecedented series of non-quinolone bacterial topoisomerase inhibitors from the Sanofi patrim
