![](images/graphics/blank.gif)
Synthesis and cytotoxic activity evaluation
-
In the last few decades, pyrazoline-based substances have emerged as potential antimicrobial and anticancer candidates. In concern with antimicrobial activity, this study aims to build a docking model to predict the structure of potential 2-pyrazoline derivatives. The cytotoxicity of some compounds was also evaluated to get insight into the structure–anticancer activity relationship of the 2- pyrazoline derivatives.
8p
vikissinger
21-12-2023
2
1
Download
-
In this study, nine ferulic and caffeic acid-based 1,2,4 and 1,3,4 oxadiazole molecular hybrids were synthesized and their cytotoxic activity was evaluated mainly against Glioblastoma (GBM) cell lines. Compounds 1 and 5 exhibited the highest inhibitory activity against three different GBM cell lines (LN229, T98G, and U87), without toxicity to healthy human mesenchymal stem cells (hMSC). In addition, their cytotoxicity was also evaluated against three additional cancer cell lines and more inhibitory results were found than GBM cell lines.
22p
lyhuyenthu
31-01-2023
6
2
Download
-
Chalcones are a class of compounds with a wide range of biological activities. In addition, derivatives based on the quinazolinone skeleton are currently of interest to research in the screening of compounds with cytotoxic effects. Compounds containing chalcone structures on the basis of quinazolinone can yield new structures with cytotoxic effects.
8p
viporsche
25-10-2022
6
2
Download
-
The 2-benzoylbenzoxazole derivatives were known for their significant biological activities such as antiproliferative activity, inhibition of FAAH enzyme (fatty acid amide hydrolase). In this study, we report a simple and efficient method for the synthesis of such compounds by the direct reaction of o-aminophenol with acetophenone catalyzed by sulfur in DMSO.
8p
vimclaren
12-10-2022
7
2
Download
-
Some thiazole derivatives bearing dithiocarbamic acid esters were synthesized in order to investigate their anticandidal activity and cytotoxicity. The structures of the obtained final compounds (6a–j) were confirmed by spectral data (IR, 1H NMR, 13C NMR, and MS) and elemental analysis. The anticandidal activity of the compounds was determined (6a–j) using the microbroth dilution method and their cytotoxicity was evaluated according to the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay against normal cells.
10p
langthannam
29-12-2021
6
0
Download
-
Several novel thiazolylpyrazoline derivatives were synthesized by reacting substituted 3,5-diaryl-1-thiocarbamoyl-2-pyrazolines with phenacylbromides. The structures of the synthesized compounds were confirmed by IR, 1 H NMR, 13 C NMR, and MS spectral data.
14p
langthannam
29-12-2021
6
0
Download
-
Novel 1-substituted 3-(p-isopropylphenyl)-5-phenylformazans (3a–g) were synthesized and characterized by elemental analysis, 1H NMR, and FT-IR techniques and UV-visible spectroscopy. Antiproliferative activities of 3a–g against HeLa and C6 cells were determined using the BrdU cell proliferation ELISA assay. 5-Florouracil was used as the positive control. The effects of substituents (–H, –CH3, and –I) and their positions (ortho, meta, and para) on the antiproliferative activities were evaluated.
9p
tudichquannguyet
29-11-2021
8
1
Download
-
Mn(II), Co(II), Ni(II), Cu(II), and Zn(II) transition metal complexes of 2-hydroxy-5-[(E)-(4-phenyl) diazenyl] benzaldehyde oxime and 2-hydroxy-5-[(E)-(4-nitrophenyl) diazenyl] benzaldehyde oxime ligands were synthesized and characterized through NMR, IR, ESI mass, and UV analysis. DNA binding abilities of the complexes were revealed using a UV-Vis spectrophotometer with the absorption titration and competitive binding techniques. Hydrolytic and oxidative DNA cleavage activities under different conditions were also proved.
20p
tudichquannguyet
29-11-2021
9
1
Download
-
A series of new thiazole-hydrazones (3a–3n) were synthesized, characterized, and screened for their hMAOA and hMAO-B inhibitory activity by an in vitro fluorometric method. Selectivity indexes (SIs) were expressed as IC50 (MAO-A) / IC50 (MAO-B). Compound 3f showed promising hMAO-A inhibition with an IC50 value of 1.20 µM and displayed a very significant SI of 0.04 towards hMAO-A. The mechanism of hMAO-A inhibition was investigated by enzyme kinetics using Lineweaver–Burk graphics.
15p
tudichquannguyet
29-11-2021
8
0
Download
-
We report herein the synthesis, characterization, and cytotoxicity evaluations of some newer oxadiazole and triazole analogues (5a–j). The cytotoxicity of all the title compounds were evaluated as per the National Cancer Institute protocol in a one-dose assay (10 µM) on nine different panels of 59 cancer cell lines. 2-{5-[(2,4-Dichlorophenoxy)methyl]- 1,3,4-oxadiazol-2-yl}phenol (5e) showed the maximum cytotoxicity among the series of ten compounds. The cytotoxicity of 5e was comparable to that of the standard anticancer drug, 5-fluorouracil, and better than that of imatinib.
18p
tudichquannguyet
29-11-2021
9
1
Download
-
A series of novel halogenated 3-hydroxyflavones (3HFs) were prepared by reacting halogenated hydroxyacetophenones with the appropriate aromatic aldehyde. Glycosylation of 3HFs with acetobromoglucose and deprotection of the acetyl protective groups afforded the desired 3-O-flavonoids glycosides in satisfactory yields. All the prepared compounds were tested for their cytotoxic activity against HCT-116, MCF-7, and OVCAR-3 human cancer cell lines. The 3HFs exhibited higher cytotoxic activities compared with the glycosylated flavonoids.
11p
tudichquannguyet
29-11-2021
12
1
Download
-
Novel methylene-tethered tetrahydroquinolines (THQs) and cyclopenta[b]pyridines were synthesized by onepot multicomponent reactions of Mannich bases, enolizable ketones, and NH4 OAc in water by an environmentally friendly K-10 montmorillonite clay-catalyzed reaction.
18p
tudichquannguyet
29-11-2021
9
0
Download
-
In this study, silver nanoparticle (AgNP) synthesis was carried out using Onosma sericeum Willd. aqueous extract for the first time, with a simple, economical, and green method without the need for any other organic solvent or external reducing or stabilizing agent. A variety of AgNPs, all of different particle sizes, were synthesized by controlling the silver ion concentration, extract volume, temperature, and pH. It was determined that the optimum conditions for AgNP synthesis were 1 mM AgNO3 , pH 8, 25 °C, 20 g/200 mL extract, silver nitrate, and extract ratio 5:1 (v/v).
16p
tudichquannguyet
29-11-2021
10
1
Download
-
In this study, a group of 4-substituted benzoyltaurinamide derivatives were designed, synthesized, and investigated for their anticancer activity against three cancer cell lines and one nontumorigenic cell line by MTT assay. Among the final compounds, methoxyphenyl derivatives 14, 15, 16 were found to be effective against all the tested cancerous cell lines with promising selectivity. The most active compounds were further evaluated to determine the molecular mechanism of their anticancer activity by using western blot assay and the Annexin V-FITC/PI test.
20p
tudichquannguyet
29-11-2021
8
0
Download
-
In this study, hydroxy benzoin (1-7), benzil (8-14), and benzoin/benzil-O-β-D-glucosides (15-25) were synthesized to investigate their biological activities. An efficient method for synthesizing hydroxy benzoin compounds (1-7) was prepared from four different benzaldehydes using an ultrasonic bath. Then, antioxidant (FRAP, CUPRAC, and DPPH), antimicrobial (3 Gram (-), 4/6 Gram (+), one tuberculosis and one fungus), and enzyme inhibition (acetylcholinesterase, butyrylcholine esterase, tyrosinase, α-amylase, and α- glucosidase) for the all synthesized compounds (1-25) were evaluated.
17p
tudichquannguyet
29-11-2021
13
1
Download
-
In search of effective antimicrobial and cytotoxic agents, a series of indole hybridized diazenyl derivatives (DS-1 to DS-21) was efciently prepared by condensation of diazotized p-aminoacetophenone with indole or nitroindole followed by reaction with different aromatic/heteroaromatic amines of biological significance.
18p
vijiraiya2711
27-05-2020
11
1
Download
-
A series of diamides derivatives containing nicotinamide unit were designed, synthesized and evaluated for their potential cytotoxic activities against human cancer cell lines.
9p
vijiraiya2711
27-05-2020
10
1
Download
-
The synthesis of new thiazole derivatives is very important because of their diverse biological activities. Also , many drugs containing thiazole ring in their skeletons are available in the market such as Abafungin, Acotia‑ mide, Alagebrium, Amiphenazole, Brecanavir, Carumonam, Cefepime, and Cefmatilen.
9p
vijiraiya2711
27-05-2020
12
1
Download
-
Prodrugs, the inert derivatives of existing drugs have successfully contributed to the modification of their physicochemical properties. The improved antimicrobial potential due to enhanced lipophilicity of some of the synthesized prodrugs of antibacterial agents by various schemes has already been reported. In the current study, synthesis, characterization, and biological evaluation of some more lipid based prodrugs/- compounds of ciprofloxacin and norfloxacin has been carried out.
8p
trinhthamhodang1
16-11-2019
28
2
Download
-
The incidence of fungal infections is considered a serious public health problem worldwide. The limited number of antimycotic drugs available to treat human and animal mycosis, the undesirable side effects and toxicities of the currently available drugs, and the emergence of fungal resistance emphasizes the urgent need for more effective antimycotic medicines. In this paper, we describe a rapid, simple, and efficient synthetic route for preparation of the antifungal agent butenafine on a multigram scale.
11p
trinhthamhodang1
14-11-2019
13
0
Download
CHỦ ĐỀ BẠN MUỐN TÌM
![](images/graphics/blank.gif)