151135-64-7

Upstream product

• 104-15-4 toluene-4-sulfonic acid 
• 151135-03-4 (E)-1-(4-(allyloxy)phenyl)-3-(2,4-dimethoxyphenyl)prop-2-en-1-one 
• 123-08-0 4-hydroxy-benzaldehyde 
• 829-20-9 2',4'-dimethoxyacetophenone 
• 613-45-6 2,4-Dimethoxybenzaldehyde 
• 2079-53-0 1-(4-(allyloxy)phenyl)ethanone 
• 99-93-4 4-Hydroxyacetophenone 

Downstream Products

• 119425-89-7 3-(2,4-dimethoxyphenyl)-1-(4-hydroxyphenyl)-1-propanone 

Relevant academic research and scientific papers

New class of hybrids based on chalcone and melatonin: a promising therapeutic option for the treatment of colorectal cancer

Considering that conventional chemotherapy provides only a limited increase of overall survival for patients with colorectal cancer (CRC), and resistance is a major cause of therapeutic failure, the emergence of new therapies is needed. Development of dif

Synthesis and anticancer activity of chalcone–quinoxalin conjugates

Two series of quinoxaline–chalcone conjugates have been prepared by aldolic condensation and aromatic nucleophilic substitution reaction, and their anticancer activity against three cancer cell lines including benign prostatic hyperplasia epithelial cell (BPH-1), neuron-like rat pheochromocytoma cell line (PC12) and human breast cancer cell line (MCF-7) were evaluated in?vitro. All of the synthesized compounds exhibited moderate to good activity against the cancer cell lines selected. Particularly, Compound A5 showed the excellent potent activity against BPH-1 and MCF-7 with IC50 values of 10.4 and 9.1 μM, respectively, which is similar to doxorubicin (14.1 and 9.2 μM, respectively). As well as compound B6 exhibited most excellent activity toward PC12 with IC50 values of 16.4 μM. Compound A10 exhibited 55.4, 36.8 and 54.5 folds higher selectivity for BPH-1, PC12 and MCF-7 cells than for HEK-293 cell, respectively. In addition, theoretical biological activities of compounds A5 and A10 were evaluated by SwissADME.

Synthesis and spectroscopic characterizations of hexakis[(1-(4′-oxyphenyl)-3-(substituted-phenyl)prop-2-en-1-one)]cyclotriphosphazenes: their in vitro cytotoxic activity, theoretical analysis and molecular docking studies

The hexachlorocyclotriphosphaze compound (N3P3Cl6, HCCP) was reacted with excess (E)-(1-(4′-oxyphenyl)-3-(substituted-phenyl)prop-2-en-1-ones (2-11) to produce hexakis[(1-(4-oxyphenyl)-3-(substituted-phenyl)prop-2-en-1-one

Synthesis and antibacterial evaluation of novel chalcone derivatives containing a benzothiazole scaffold

Abstract: A series of novel chalcone derivatives containing a benzothiazole scaffold were synthesized to develop novel antibacterial agents for solving the problem of drug resistance. Most compounds exhibited excellent antibacterial activity against Xanthomonas oryzae pv. Oryzae (Xoo), Xanthomonas axonopodis pv. Citri (Xac), and Ralstonia solanacearum (Rs) compared to a reference drug, bismerthiazol. The results indicated that chalcone derivatives containing a benzothiazole scaffold merit more research as promising antibacterial agents. Graphical abstract: [Figure not available: see fulltext.].

Novel chalcone derivatives containing a 1,2,4-triazine moiety: Design, synthesis, antibacterial and antiviral activities

A series of novel chalcone derivatives containing the 1,2,4-triazine moiety were synthesized and their structures were confirmed by 1H NMR, 13C NMR and elemental analyses. Antiviral bioassays revealed that most of the compounds exhibited good antiviral activity against tobacco mosaic virus (TMV) at a concentration of 500 μg mL-1. The designated compound 4l was 50% effective in terms of curative and protective activities against TMV with 50% effective concentrations (EC50) of 10.9 and 79.4 μg mL-1, which were better than those of ningnanmycin (81.4 and 82.2 μg mL-1). Microscale thermophoresis (MST) also showed that the binding of compound 4l to coat protein (TMV-CP) yielded a Kd value of 0.275 ± 0.160 μmol L-1, which was better than that of ningnanmycin (0.523 ± 0.250 μmol L-1). At the same time, molecular docking studies for 4l with TMV-CP (PDB code:1EI7) showed that the compound was embedded well in the pocket between the two subunits of TMV-CP. Meanwhile, compound 4a demonstrated excellent antibacterial activities against Ralstonia solanacearum (R. solanacearum), with an EC50 value of 0.1 μg mL-1, which was better than that of thiodiazole-copper (36.1 μg mL-1) and bismerthiazol (49.5 μg mL-1). The compounds act by causing folding and deformation of the bacterial cell membrane as observed using scanning electron microscopy (SEM). The chalcone derivatives thus synthesized could become potential alternative templates for novel antiviral and antibacterial agents.

Synthesis and antiviral bioactivity of novel chalcone derivatives containing purine moiety

A series of novel chalcone derivatives containing purine moiety was designed and synthesized, and their antiviral activities against cucumber mosaic virus (CMV) and tobacco mosaic virus (TMV) were evaluated in vivo. Bioactivity assays indicated that some compounds showed good antiviral activities against CMV and TMV. It is worth mentioning that compounds 3o, 3s, 3w, and 3x exhibited excellent curative activity against CMV, with EC50 values of 301.1 μg/mL, 315.7 μg/mL, 282.3 μg/mL, 230.5 μg/mL, respectively, which were better than that of Dufulin (373.7 μg/mL) and Ribavirin (726.3 μg/mL). In addition, the fluorescence spectroscopy experiment results showed that compound 3o showed strong combining capacity to tobacco mosaic virus coat protein.

Novel trans-Ferulic Acid Derivatives Containing a Chalcone Moiety as Potential Activator for Plant Resistance Induction

A series of novel trans-ferulic acid derivatives containing a chalcone moiety were designed and synthesized to induce plant resistance. Antiviral activities of the compounds were evaluated. Bioassay results demonstrated that compounds F3, F6, F17, and F27 showed remarkable curative, protective, and inactivating activities against tobacco mosaic virus (TMV). With a 50% effective concentration (EC50) value of 98.78 μg mL-1, compound F27 exhibited the best protective activity compared with trans-ferulic acid (328.6 μg mL-1), dufulin (385.6 μg mL-1), and ningnanmycin (241.3 μg mL-1). This protective ability was associated with potentiation of defense-related enzyme activity and activation of photosynthesis of tobacco at an early stage. This notion was confirmed by up-regulated expression of stress responses and photosynthesis regulating proteins. This work revealed that F27 can induce resistance and enhance plant tolerance to TMV infection. Hence, F27 can be considered as a novel activator for inducing plant resistance.

Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity

A new series of monomer and dimer derivatives of dihydroartemisinin (DHA) containing substituted chalcones as a linker were synthesized and investigated for their cytotoxicity in human cancer cell lines HL-60 (leukemia), Mia PaCa-2 (pancreatic cancer), PC

Synthesis, antiviral bioactivity of novel 4-thioquinazoline derivatives containing chalcone moiety

A series of novel 4-thioquinazoline derivatives containing chalcone moiety were designed, synthesized and systematically evaluated for their antiviral activity against TMV. The bioassay results showed that most of these compounds exhibited moderate to good anti-TMV activity. In particular, compounds M2 and M6 possessed appreciable protection activities against TMV in vivo, with 50% effective concentration (EC50) values of 138.1 and 154.8 μg/mL, respectively, which were superior to that of Ribavirin (436.0 μg/mL). The results indicated that chalcone derivatives containing 4-thioquinazoline moiety could effectively control TMV. Meanwhile, the structure-activity relationship (SAR) of the target compounds, studied using the three-dimensional quantitative structure-activity relationship (3D-QSAR) method of comparative molecular field analysis (CoMFA) based on the protection activities against TMV, demonstrated that the CoMFA model exhibited good predictive ability with the cross-validated q2 and non-cross-validated r2 values of 0.674 and 0.993, respectively. Meanwhile, the microscale thermophoresis (MST) experimental showed that the compound M6 may interaction with the tobacco mosaic virus coat protein (TMV CP).

Synthesis and bioevaluation of 3-(substitutedphenyl)-1-(4-hydroxyphenyl)-2-propen-1-ones and their carbamate derivatives against root - knot nematode (meloidogyne javanica)

Synthesis of 3-(4-chloro/methyl/nitro/methoxy/3,4,5-trimethoxy/2,4-dichloro/ 4-bromo/ 3, 4-dimethoxy/ 2, 4-dimethoxy/ 3-bromo/ 2-chloro/ 2-methoxy phenyl)-1-(4-hydroxyphenyl)-2-propen-1-one (14-25) has been carried out from substituted benzaldehyde (1-12)