22248-31-3Relevant 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
Design, synthesis, characterization and in silico molecular docking studies and in vivo anti-inflammatory activity of pyrazoline clubbed thiazolinone derivatives
Chawla, Pooja A.,Kulshreshtha, Mayank,Kumar, Yogesh,Shukla, Karuna Shanker,Singh, Deepak Kumar,Ved, Akash
, p. 735 - 748 (2021/10/01)
The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities, including inflammatory action.
Synthesis and biological evaluation of chalcone, dihydrochalcone, and 1,3-diarylpropane analogs as anti-inflammatory agents
Vijaya Bhaskar Reddy, Mopur,Hung, Hsin-Yi,Kuo, Ping-Chung,Huang, Guan-Jhong,Chan, Yu-Yi,Huang, Shiow-Chyn,Wu, Shwu-Jen,Morris-Natschke, Susan L.,Lee, Kuo-Hsiung,Wu, Tian-Shung
supporting information, p. 1547 - 1550 (2017/03/17)
Twenty-one chalcones were prepared via aldol condensation and subsequent reduction of these compound led to the corresponding dihydrochalcone and 1,3-diphenylpropane derivatives. The synthetic products were examined for their effects on NO inhibition in L
Syntheses of 2-methoxyestradiol and eugenol template based diarylpropenes as non-steroidal anticancer agents
Pathak, Vinay,Ahmad, Imran,Kahlon, Amandeep Kaur,Hasanain, Mohammad,Sharma, Sandeep,Srivastava, Kishore K.,Sarkar, Jayanta,Shankar, Karuna,Sharma, Ashok,Gupta, Atul
, p. 35171 - 35185 (2014/11/07)
Syntheses of 2-methoxyestradiol (1) and eugenol (6) template based conformationally flexible and rigid diarylpropenes, 14(a-l) and 20(a-e), as nonsteroidal anticancer agents have been performed. The synthesized compounds were evaluated for their anticance
Microwave synthesis, characterization and bio-efficacy evaluation of novel chalcone based 6-carbethoxy-2-cyclohexen-1-one and 2H-indazol-3-ol derivatives
Shakil,Singh, Manish K.,Sathiyendiran,Kumar,Padaria, Jasdeep C.
, p. 120 - 131 (2013/03/14)
Novel chalcone based 6-carbethoxy-2-cyclohexen-1-one and 2H-indazol-3-ol derivatives were synthesized and characterized by using spectral techniques like IR, 1H NMR, 13C NMR, COSY, DEPT, and GC-MS. All these compounds were screened for anti-fungal, anti-bacterial and anti-oxidant activity. Cyclohexenone derivatives, in general, showed better anti-fungal and anti-bacterial activity than parent chalcones. Whereas, all the Indazole derivatives showed very good anti-oxidant activity and some were also found to be active as anti-bacterial agent. Among the screened compounds, 15 was found to be most active as anti-fungal agent (against Rhizoctonia solani, LC 50 = 2.36 μg mL-1), 15b was found to be most active anti-bacterial agent (against Klebsiella pneumonia, MIC = 24.68 μg mL -1) and 14b emerged as most active anti-oxidant (IC50 = 19.81 μg mL-1).
Synthesis, cytotoxic properties and tubulin polymerization inhibitory activity of novel 2-pyrazoline derivatives
Abdel-Aziz, Mohamed,Aly, Omar M.,Khan, Sabine S.,Mukherjee, Kamalika,Bane, Susan
scheme or table, p. 535 - 548 (2012/09/08)
A series of novel 1-(3',4',5'-trimethoxybenzoyl)-3,5-diarylpyrazoline derivatives were synthesized and evaluated for their cytotoxic properties on different cancer cell lines and tubulin polymerization inhibitory activity. Compounds 6d and 6e exhibited re
Investigation of chalcones and benzochalcones as inhibitors of breast cancer resistance protein
Juvale, Kapil,Pape, Veronika F.S.,Wiese, Michael
experimental part, p. 346 - 355 (2012/03/09)
Breast cancer resistance protein (BCRP/ABCG2) belongs to the ATP binding cassette family of transport proteins. BCRP has been found to confer multidrug resistance in cancer cells. A strategy to overcome resistance due to BCRP overexpression is the investigation of potent and specific BCRP inhibitors. The aim of the current study was to investigate different multi-substituted chalcones for their BCRP inhibition. We synthesized chalcones and benzochalcones with different substituents (viz. OH, OCH3, Cl) on ring A and B of the chalcone structure. All synthesized compounds were tested by Hoechst 33342 accumulation assay to determine inhibitory activity in MCF-7 MX and MDCK cells expressing BCRP. The compounds were also screened for their P-glycoprotein (P-gp) and Multidrug resistance-associated protein 1 (MRP1) inhibitory activity in the calcein AM accumulation assay and were found to be selective towards inhibition of BCRP. Substituents at position 2′ and 4′ on chalcone ring A were found to be essential for activity; additionally there was a great influence of substituents on ring B. Presence of 3,4-dimethoxy substitution on ring B was found to be optimal, while presence of 2- and 4-chloro substitution also showed a positive effect on BCRP inhibition.
Evaluation and discovery of novel synthetic chalcone derivatives as anti-inflammatory agents
Wu, Jianzhang,Li, Jianling,Cai, Yuepiao,Pan, Yong,Ye, Faqing,Zhang, Yali,Zhao, Yunjie,Yang, Shulin,Li, Xiaokun,Liang, Guang
experimental part, p. 8110 - 8123 (2012/01/07)
Major anti-inflammatory agents, steroids and cyclooxygenase, were proved to have serious side effects. Here, a series of chalcone derivatives were synthesized and screened for anti-inflammatory activities. QSAR study revealed that the presence of electron-withdrawing groups in B-ring and electron-donating groups in A-ring of chalcones was important for inhibition of LPS-induced IL-6 expression. Further, compounds 22, 23, 26, 40, and 47 inhibited TNF-α and IL-6 release in a dose-dependent manner and decreased LPS-induced TNF-α, IL-1β, IL-6, IL-12, and COX-2 mRNA production. Mechanistically, compounds 23 and 26 interfered with JNK/NF-κB signaling and dose-dependently prevented ERK and p38 activation. In addition, 23 and 26 exhibited a significant protection against LPS-induced death and were able to block high glucose-activated cytokine profiles in macrophages. Together, these data show a series of anti-inflammatory chalcones with potential therapeutic effects in inflammatory diseases.
The synthesis of indanones related to combretastatin A-4 via microwave-assisted Nazarov cyclization of chalcones
Lawrence, Nicholas J.,Armitage, E. Simon M.,Greedy, Benjamin,Cook, Darren,Ducki, Sylvie,McGown, Alan T.
, p. 1637 - 1640 (2007/10/03)
A fast and efficient microwave-assisted synthesis of combretastatin A-4-like indanones has been developed. Microwave irradiation provides a useful alternative to traditional heating techniques to promote the TFA-catalyzed Nazarov cyclization of chalcones.
Discovery of fluorescent cyanopyridine and deazalumazine dyes using small molecule macroarrays
Bowman, Matthew D.,Jacobson, Megan M.,Blackwell, Helen E.
, p. 1645 - 1648 (2007/10/03)
Small molecule macroarrays of cyanopyridines and deazalumazines were generated in high purities via spatially addressed synthesis on planar cellulose supports. Examination of the spectral properties of the heterocycles both on and off of the planar suppor
