93877-79-3Relevant academic research and scientific papers
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity
Abdel-Halim, Mohammad,Sigler, Sara,Racheed, Nora A. S.,Hefnawy, Amr,Fathalla, Reem K.,Hammam, Mennatallah A.,Maher, Ahmed,Maxuitenko, Yulia,Keeton, Adam B.,Hartmann, Rolf W.,Engel, Matthias,Piazza, Gary A.,Abadi, Ashraf H.
supporting information, p. 4462 - 4477 (2021/05/04)
A ligand-based approach involving systematic modifications of a trisubstituted pyrazoline scaffold derived from the COX2 inhibitor, celecoxib, was used to develop novel PDE5 inhibitors. Novel pyrazolines were identified with potent PDE5 inhibitory activit
Molecular docking of 4-ehoxychalcones on oxidoreductase/pirin inhibitors and cytotoxic evaluation on breast/skin cancer cell lines
Harshitha, Kishori Ramachandra,Sarojini, Balladka Kunhanna,Narayana, Badiadka,Lobo, Anupam Glorious,Kalal, Bhuvanesh Sukhlal
, p. 1245 - 1260 (2020/10/06)
Background: The role of α, β unsaturated propenone derivatives, has attracted the chemists for its biological importance. An attempt is made to reveal the interaction between breast and skin cancer cell lines with the help of molecular docking studies. Ob
Antimalarial alkoxylated and hydroxylated chalones: Structure-activity relationship analysis
Liu,Wilairat,Go
, p. 4443 - 4452 (2007/10/03)
Chalcones with 2′,3′,4′-trimethoxy, 2′,4′-dimethoxy, 4′-methoxy, 4′-ethoxy, 2′,4′-dihydroxy, and 4′-hydroxy groups on ring B were synthesized and evaluated in vitro against Plasmodium falciparum (K1) in a [3H] hypoxanthine uptake assay. The other ring A was quinoline, pyridine, naphthalene, or phenyl rings with electron-donating or electron-withdrawing substituents of varying lipophilicities. Trimethoxy 6 and 27, dimethoxy 7, 8, 29, and methoxy 31 analogues had good in vitro activities (IC50 5μM). 3-Quinolinyl ring A derivatives were well represented among the active compounds. Hydroxylated chalcones were less active than the corresponding alkoxylated analogues. When evaluated in vivo, 8 and 208 were comparable to chloroquine in extending the lifespan of infected mice. Multivariate data analysis showed that in vitro activity was mainly determined by the properties of ring B. Quantitative structure - activity relationship models with satisfactory predictive ability were obtained for various B ring chalcones using projections to latent structures. A model with good predictability was proposed for 19 active chalcones. Size and hydrophobicity were identified as critical parameters.
Improved microwave-induced synthesis of chalcones and related enones
Gupta, Rajive,Gupta, Avinash K.,Paul, Satya,Kachroo, P. L.
, p. 61 - 62 (2007/10/02)
Various chalcones and related enones have been synthesised in unsealed vessels in a domestic microwave oven.Considerable increase in the reaction rate has been observed with better yields.
Synthesis and antimicrobial activity of 1-(4-chlorophenyl)-3-(4-methoxy/3,4-dimethoxyphenyl)propan-1,3-diones and their 2-analogs
Singh, Rajvir,Malik, Om Parkash
, p. 455 - 459 (2007/10/02)
The condensation of substituted acetophenones 1-5 with 4-methoxy- or 3,4-dimethoxy-benzaldehyde (6,7) in ethanolic NaOH gives the corresponding substituted 2-propen-1-ones (8-17) which on bromination yields substituted propan-1-ones (18-27).Refluxing of 1
