79492-48-1

Upstream product

• 2309-48-0 1,3-di(thiophen-2-yl)propenone 
• 109-77-3 malononitrile 
• 98-03-3 thiophene-2-carbaldehyde 
• 88-15-3 2-Acetylthiophene 
• 933920-41-3 2-bromo-4,6-bis(2-thienyl)-3-pyridinecarbonitrile 
• 42811-88-1 (E)-1,3-di(thiophen-2-yl)prop-2-en-1-one 
• 28162-32-5 2-(2-thienyl)-1-cyanoacrylonitrile 
• 554-14-3 2-Methylthiophene 

Relevant academic research and scientific papers

Green Synthesis, Cytotoxicity and Antimicrobial Activities of Some New Pyrazolines, Pyrimidines and Naphthyridines Based on 1,3-Di(thien-2-yl)prop-2-en-1-one Using Choline Chloride-Urea Mixture As A Deep Eutectic Solvent

An efficient and facile green synthesis of chalcone derivatives 1a-d was achieved by treatment of aromatic aldehydes with 2-acetylthiophene in the presence of choline chloride-urea mixture as a deep eutectic solvent. Chalcone 1a was used as a reactive key precursor to design a series of bio-active heterocycles such as pyrimidine, pyrazoline, pyridine, pyridopyrimidine and naphthyridine. The Structural formula of derivatives were confirmed and characterized by their elemental analyses and spectral data (IR, MS, 1H NMR, 13C NMR). In addition, the synthesized derivatives were evaluated for their antimicrobial activities, it was found that compounds 3, 8 and 9a exhibited potent antifungal activity in comparison with the standard drug. Cytotoxicity against breast cancer (MCF7) was screened also and most compounds showed low to moderate activity. The results of the viral screening against HBV of selected compounds indicated that compounds (9b, 15), 8, (3, 6), and 5 showed moderate viral replication inhibition.

Eco-friendly synthesis of novel cyanopyridine derivatives and their anticancer and PIM-1 kinase inhibitory activities

Targeting Pim-1 kinase recently proved to be profitable for conquering cancer proliferation. In the current study, we report the design, synthesis and biological evaluation of two novel series of 2-amino cyanopyridine series (5a-g) and 2-oxocyanopyridine series (6a-g) targeting Pim-1 kinase. All of the newly synthesized compounds were evaluated for their in?vitro anticancer activity against a panel of three cell lines, namely, the liver cancer cell line (HepG2), the colon cancer cell line (HCT-116) and the breast cancer cell line (MCF-7). Most of the compounds showed good to moderate anti-proliferative activity against HepG2 and HCT-116?cell lines while only few compounds showed significant cytotoxic activity against MCF-7?cell line. Further, the Pim-1 kinase inhibitory activity for the two series was?evaluated where most of the tested compounds showed marked Pim-1 kinase inhibitory activity (26%–89%). Moreover, determination of the IC50 values unraveled very potent molecules in the submicromolar range where compound 6c possessed an IC50 value of 0.94?μM. Moreover, apoptosis studies were conducted on the most potent compound 6c to evaluate the proapoptotic potential of our compounds. Interestingly, it induced the level of active caspase 3 and boosted the Bax/Bcl2 ratio 22704 folds in comparison to the control. Finally, a molecular docking study was conducted to reveal the probable interaction with the Pim-1 kinase active site.

Synthesis, bioassay, and molecular field topology analysis of diverse vasodilatory heterocycles

A diverse training set composed of 76 in-house synthesized and 61 collected from the literature was subjected to molecular field topology analysis. This resulted in a high-quality quantitative structure-activity relationships model (R2 = 0.932,

2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2a adenosine receptor antagonists

A2A adenosine receptor antagonists usually have bi- or tricyclic N aromatic systems with varying substitution patterns to achieve desired receptor affinity and selectivity. Using a pharmacophore model designed by overlap of nonxanthine type of previously known A2A antagonists, we synthesized a new class of compounds having a 2-amino nicotinonitrile core moiety. From our data, we conclude that the presence of at least one furan group rather than phenyl is beneficial for high affinity on the A2A adenosine receptor. Compounds 39 (LUF6050) and 44 (LUF6080) of the series had Ki values of 1.4 and 1.0 nM, respectively, with reasonable selectivity toward the other adenosine receptor subtypes, A1, A 2B, and A3. The high affinity of 44 was corroborated in a cAMP second messenger assay, yielding subnanomolar potency for this compound.

Synthesis and antibacterial properties of new dithienyl containing pyran, pyrano[2,3-b] pyridine, pyrano[2,3-d]pyrimidine and pyridine derivatives

Some new pyran 3,8; pyrano[2,3-b]pyridine 4; pyrano[2,3-d] pyrimidine 5,6,7 and 9; pyridine 10-14 derivatives have been prepared. The structure of all the new compounds have been established on the basis of elemental analyses and spectroscopic data. All t

Malononitriles and Cyanoesters: Part VII- Diaryl- and Dithienylpropenones and -cyanopyridines and Their Molluscicidal Activity

2-Amino-3-cyano-4,6-disubstituted-pyridines (6) and 3-cyano-4,6-disubstituted-pyridin-2-ones (10) are obtained by reacting the corresponding propenones (1) with malononitrile and ethyl cyanoacetate, respectively, in the presence of ammonium acetate.The compounds (6) and (10) can be readily obtained by reacting the corresponding ylidene-malononitriles (8) and -cyanoesters (9) with the appropriate ketone.Molluscicidal activity of the compounds is also discussed.