59887-89-7Relevant articles and documents
Anti-HIV agents. Part 55: 3′R,4′R-Di-O-(-)-camphanoyl-2′,2′- dimethyldihydropyrano[2,3-f]chromone (DCP), a novel anti-HIV agent
Yu, Donglei,Brossi, Arnold,Kilgore, Nicole,Wild, Carl,Allaway, Graham,Lee, Kuo-Hsiung
, p. 1575 - 1576 (2003)
3′R,4′R-Di-O-(-)-camphanoyl-2′,2′- dimethyldihydropyrano[2,3-f]chromone (DCP) (2) was designed and synthesized on the basis of a structure-activity relationship study of 3′R,4′R-di-O-(-)-camphanoyl-(+)-cis-khellactone DCK (1) and its analogues. DCP (2), a pyranochromone, and DCK (1), a pyranocoumarin, have different skeletons. Compound 2 showed potent in vitro inhibition of HIV-1 replication in H9 lymphocyte cells with an EC50 of 6.78×10-4 μM and TI of 14,500. These values are comparable with those for DCK (1) and better than those of AZT in the same assay.
Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis
Chu, Zhaoxing,Xu, Qinlong,Zhu, Qihua,Ma, Xiaodong,Mo, Jiajia,Lin, Gaofeng,Zhao, Yan,Gu, Yuanfeng,Bian, Lincui,Shao, Li,Guo, Jing,Ye, Wenfeng,Li, Jiaming,He, Guangwei,Xu, Yungen
, (2021/02/03)
In this work, a series of structurally novel benzoxaborole derivatives were designed, synthesized and biologically evaluated as PDE4 inhibitors for battling atopic dermatitis (AD). Among them, the majority exhibited superior PDE4B inhibitory activities to that of the lead compound Crisaborole, an approved PDE4 inhibitor. In particular, 72, the most potent PDE4B inhibitor throughout this series, displayed 136-fold improved enzymatic activity (IC50 = 0.42 nM) as compared to Crisaborole (IC50 = 57.20 nM), along with favorable isoform specificity. In the phorbol ester (PMA)-induced mouse ear oedema model, 72 exerted remarkably greater efficacy than Crisaborole at the same dosage (P 0.05). Moreover, the ointment of 72 exerted dramatically enhanced therapeutic potency than the ointment of Crisaborole (P 0.05) in the calcipotriol-induced mouse AD model. In addition to the potent in vitro and in vivo activity, 72 displayed favorable safety in the repeated oral dose toxicity study and did not exhibit phototoxicity. With the above attractive biological performance, 72 is worthy of further functional investigation as a novel anti-AD therapeutic agent.
Chromone derivatives bearing pyridinium moiety as multi-target-directed ligands against Alzheimer's disease
Abdpour, Shahin,Jalili-Baleh, Leili,Nadri, Hamid,Forootanfar, Hamid,Bukhari, Syed Nasir Abbas,Ramazani, Ali,Ebrahimi, Seyed Esmaeil Sadat,Foroumadi, Alireza,Khoobi, Mehdi
, (2021/03/14)
A new serise of 7-hydroxy-chromone derivatives bearing pyridine moiety were synthesized, and evaluated as multifunctional agents against Alzheimer's disease (AD). Most of the compounds were good AChE inhibitors (IC50 = 9.8–0.71 μM) and showed remarkable BuChE inhibition activity (IC50 = 1.9–0.006 μM) compared with donepezil as the standard drug (IC50 = 0.023 and 3.4 μM). Compounds 14 and 10 showed the best inhibitory activity toward AChE (IC50 = 0.71 μM) and BuChE (IC50 = 0.006 μM), respectively. The ligand–protein docking simulations and kinetic studies revealed that compound 14 and 10 could bind effectively to the peripheral anionic binding site (PAS) of the AChE and BuChE through mixed-type inhibition. In addition, the most potent compounds showed acceptable neuroprotective activity on H2O2- and Aβ-induced.neurotoxicity in PC12 cells, more than standard drugs. The compounds could block effectively self- and AChE-induced Aβ aggregation. All the results suggest that compounds 14 and 10 could be considered as promising multi-target-directed ligands against AD.
