29124-57-0Relevant articles and documents
Structure-antiplatelet activity relationships of novel ruthenium (ii) complexes: Investigation of its molecular targets
Hsia, Chih-Hsuan,Jayakumar, Thanasekaran,Sheu, Joen-Rong,Tsao, Shin-Yi,Velusamy, Marappan,Hsia, Chih-Wei,Chou, Duen-Suey,Chang, Chao-Chien,Chung, Chi-Li,Khamrang, Themmila,Lin, Kao-Chang
, (2018)
The regulation of platelet function by pharmacological agents that modulate platelet signaling has proven to be a positive approach to the prevention of thrombosis. Ruthenium complexes are fascinating for the development of new drugs, as they possess numerous chemical and biological properties. The present study aims to evaluate the structure-activity relationship (SAR) of newly synthesized ruthenium (II) complexes, TQ-1, TQ-2 and TQ-3 in agonists-induced washed human platelets. Silica gel column chromatography, aggregometry, immunoblotting, NMR, and X-ray analyses were performed in this study. Of the three tested compounds, TQ-3 showed a concentration (1–5 μM) dependent inhibitory effect on platelet aggregation induced by collagen (1 μg/mL) and thrombin (0.01 U/mL) in washed human platelets; however, TQ-1 and TQ-2 had no response even at 250 μM of collagen and thrombin-induced aggregation. TQ-3 was effective with inhibiting collagen-induced ATP release, calcium mobilization ([Ca2+]i) and P-selectin expression without cytotoxicity. Moreover, TQ-3 significantly abolished collagen-induced Lyn-Fyn-Syk, Akt-JNK and p38 mitogen-activated protein kinases (p38 MAPKs) phosphorylation. The compound TQ-3 containing an electron donating amino group with two phenyl groups of the quinoline core could be accounted for by its hydrophobicity and this nature might be the reason for the noted antiplatelet effects of TQ-3. The present results provide a molecular basis for the inhibition by TQ-3 in collagen-induced platelet aggregation, through the suppression of multiple machineries of the signaling pathway. These results may suggest that TQ-3 can be considered a potential agent for the treatment of vascular diseases.
Synthesis, biological evaluation and virtual screening of some acridone derivatives as potential anticancer agents
Bogan, Deanna N.,Okoro, Cosmas O.,Oyedele, Abiodun S.
, (2020)
Eleven novel acridone derivatives were synthesized and evaluated for their anticancer activity against 60 human cancer cell lines. Five compounds 8b, 8d, 8g, 8h, and 8k displayed very good in vitro antiproliferative activities well over 95% of the panels.
Repurposing an Aldolase for the Chemoenzymatic Synthesis of Substituted Quinolines
Fansher, Douglas J.,Granger, Richard,Kaur, Satinderpal,Palmer, David R. J.
, p. 6939 - 6943 (2021/06/28)
Quinoline derivatives are important natural products and pharmaceuticals, but their synthesis can be challenging due to poor yields, harsh reaction conditions, and instability of starting materials. Here we report the chemoenzymatic synthesis of quinaldic acids under mild conditions using an aldolase, trans-o-hydroxybenzylidenepyruvate hydratase-aldolase (NahE, or HBPA). A series of 2-aminobenzaldehydes derived from reduction of the corresponding nitro analogue were reacted with pyruvate in the presence of NahE to give substituted quinolines in up to 93% isolated yield. This reaction differs from the aldol condensation catalyzed by NahE in vivo, instead resembling the heterocycle formation catalyzed by its homologue, dihydrodipicolinate synthase.
Photophysics and reverse saturable absorption of cationic dinuclear iridium(iii) complexes bearing fluorenyl-tethered 2-(quinolin-2-yl)quinoxaline ligands
Cui, Peng,Kilina, Svetlana,Lu, Cuifen,Lu, Taotao,Sun, Wenfang
, p. 14309 - 14319 (2021/10/25)
The synthesis, photophysics and reverse saturable absorption of two cationic dinuclear Ir(iii) complexes bearing fluorenyl-tethered 2-(quinolin-2-yl)quinoxaline (quqo) ligands are reported in this paper. The two complexes possess intense and featureless diimine ligand localized1ILCT (intraligand charge transfer)/1π,π* absorption bands atca.330 and 430 nm, and a weak1,3MLCT (metal-to-ligand charge transfer)/1,3LLCT (ligand-to-ligand charge transfer) absorption band at >500 nm. Both complexes exhibit weak dual phosphorescence atca.590 nm and 710 nm, which are attributed to the3ILCT/3π,π* and3MLCT/3LLCT states, respectively. The low-energy3MLCT/3LLCT state also gives rise to a moderately strong triplet excited-state absorption at 490-800 nm. Because of the stronger triplet excited-state absorption than the ground-state absorption of these complexes at 532 nm, both complexes manifest a moderate reverse saturable absorption (RSA) at 532 nm for ns laser pulses. Expansion of the π-conjugation of the fluorenyl-tethered diimine ligand inIr-1causes a slight red-shift of the1ILCT/1π,π* absorption bands in its UV-vis absorption spectrum and the3MLCT/3LLCT absorption band in the transient absorption spectrum and slightly enhances the RSA at 532 nm compared to that inIr-2. This work represents the first report on dinuclear Ir(iii) complexes that exhibit RSA at 532 nm.
