scholarly journals Synthesis, In Vitro Antimicrobial and Cytotoxic Activities of Some New Pyrazolo[1,5-a]pyrimidine Derivatives

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1080 ◽  
Author(s):  
Ahmed Fouda ◽  
Hebat-Allah Abbas ◽  
Eman Ahmed ◽  
Ali Shati ◽  
Mohammad Alfaifi ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Antitumor Activities ◽  
Efficient Procedure ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Antibacterial And Antifungal ◽  
Mcf 7

A new series of pyrazole 4–7 and pyrazolo[1,5-a]pyrimidine 8–13 were synthesized by using a simple, efficient procedure, and screened for their in-vitro antimicrobial and antitumor activities. Symmetrical and asymmetrical 3,6-diarylazo-2,5,7-triaminopyrazolo[1,5-a]pyrimidine were synthesized by the conventional method and also subjected to microwave irradiation and under ultrasound conditions. The biological results revealed that most of the tested compounds proved to be active as antibacterial and antifungal agents. The antitumor activity of the synthesized compounds was evaluated against human cancer cell lines, MCF-7, HCT-116, and HepG-2, as compared with Doxorubicin as a control.

scholarly journals Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3923
Author(s):  
Adel A.-H. Abdel-Rahman ◽  
Amira K. F. Shaban ◽  
Ibrahim F. Nassar ◽  
Dina S. EL-Kady ◽  
Nasser S. M. Ismail ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Molecular Docking Study ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Mcf 7

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-−C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1, 2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24, 0.65, 0.50, and 0.93 µM, respectively, compared to roscovitine (IC50 0.394 μM). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 μM, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 µM, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.

scholarly journals Two New Cytotoxic Steroidal Alkaloids from Sarcococca Hookeriana

Molecules ◽  
2018 ◽  
Vol 24 (1) ◽  
pp. 11 ◽  
Author(s):  
Shaojie Huo ◽  
Jichun Wu ◽  
Xicheng He ◽  
Lutai Pan ◽  
Jiang Du
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Steroidal Alkaloids ◽  
X Ray ◽  
Human Cancer Cell Lines ◽  
X Ray Crystallography ◽  
Ic50 Values ◽  
Mcf 7

Two new steroidal alkaloids, named hookerianine A (1) and hookerianine B (2) were isolated from the stems and roots of Sarcococca hookeriana Baill., along with two known compounds, sarcorucinine G (3) and epipachysamine D (4). On the basis of spectroscopic methods and by comparison with literature data, their structures were determined. As well as X-ray crystallography was performed to confirm compound 4. To identify novel antitumor inhibitors, all compounds were performed a CCK-8 assay against five human cancer cell lines SW480, SMMC-7721, PC3, MCF-7 and K562 in vitro. Compound 2 exhibited moderate cytotoxic activities to all cell lines with IC50 values in the range of 5.97–19.44 μM. Compound 3 was the most effective one against SW480 and K562 cell lines with IC50 values of 5.77 and 6.29 μM, respectively.

scholarly journals In vitro anti-proliferative activity of selected nutraceutical compounds in human cancer cell lines

2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Endalkachew Nibret ◽  
Sonja Krstin ◽  
Michael Wink
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Human Cancer Cell Lines ◽  
Nutraceutical Compounds ◽  
Hct 116 ◽  
Β Carotene

Abstract Objective We investigated the anti-proliferative or cytotoxic activities of five nutraceutical compounds: allyl isothiocyanate, β-carotene, caffeine, capsaicin, and lupanine that we consume respectively, for example, from mustard seeds, carrot, coffee, pepper, and lupin seeds against cancer cell lines (human colon: HCT 116 p53 wild type, HCT 116 p53−/− and lymphoblastic: CEM/CCRF, CEM/ADR5000). Result Out of the five compounds tested in vitro, capsaicin and β-carotene were more cytotoxic than the other three compounds against the four cancer cell lines. The most potent nutraceutical compound was capsaicin and it exerted its highest cytotoxicity against HCT 116 p53−/− with IC50 value of 19.67 ± 0.06 µM. It is worth considering capsaicin for further development of anticancer drug against both colon and leukemia cancer types.

scholarly journals Anticancer and molecular docking studies of some new pyrazole-1-carbothioamide nucleosides

2019 ◽  
Vol 9 (6) ◽  
pp. 4642-4648 ◽  
Keyword(s):  
Molecular Docking ◽  
Human Cancer ◽  
Docking Study ◽  
Molecular Docking Study ◽  
Reference Drug ◽  
Human Cancer Cell Lines ◽  
Chemical Structures ◽  
Hct 116 ◽  
Mcf 7

Eight pyrazole-1-carbothioamide nucleosides were synthesized through conensation of 3-(4-aminophenyl)-pyrazole-1-carbothioamide derivative 2 with four aldoses (arabinose, mannose, glucose and galactose) and acetylation of the produced nucleosides 3a-d with acetic anhydride in pyridine at room temperature to give their corresponding acetyl derivatives 4a-d. Their chemical structures were confirmed by spectroscopic and elemental analysis. The antiproliferative activity was screened against various human cancer cell lines (MCF-7, HepG2 and HCT-116) in vitro; compound 4b showed a significant IC50 values (8.5±0.72 for MCF-7, 9.4±0.84 for HepG2 and 11.7±0.89 µg/ml for HCT-116) which were close to the reference drug 5-fluorouracil (5-FU). Molecular docking study was utilized to illustrate the ability of the more active compounds 3b and 4b to inhibit thymidylate synthase and compare the results with an antimetabolite drug used in cancer chemotherapy "Raltitrexed".

In vitro Assessment the Potential Antioxidant and Antitumor Activities of Bifidobacterium Derived Bacteriocins

2019 ◽  
Vol 9 (02) ◽  
Author(s):  
Shadan A Alwendawi
Keyword(s):  
Antioxidant Activity ◽  
Human Cancer ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Cancer Drug ◽  
Scavenging Activity ◽  
Antitumor Activities ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Nowadays there are increasing interest in using microbial bioactive peptides as therapeutic agents or as adjuvant to increase the effectiveness of available therapies, a promising approach in this line is using of probiotics secreted peptides. Bifidobacterium is one of the favorite patented probiotics genera and most of human enteric Bifidobacterium secretes bacteriocins peptides to the surroundings. Bifidobacterial – associated bacteriocins are classified as GRAS peptides, and recently were attracted attention that become a widespread research topic in various fields including cancer drug discovery development. This study was conducted to seek for antioxidant and antitumor activities of bifidobacterial – derived bacteriocins. Two bacteriocins, Bifidin B1 and Bifidin B2, were partially purified from enteric Bifidibacterium longum Bl and Bifidobacterium bifidum B2, respectively. Bifidins were physiochemically characterized in respective of thermal, pH, and storage stability. Their proteinaceous nature was confirmed. Potential antioxidant activity in terms of free radical scavenging activity was evaluated, both Bifidins exhibited antioxidant activity, the highest percentage scavenging activity against DPPH was 70.55±0.2673 %, recorded for Bifidin B1, and was followed by 68.1 ±1.753% scavenging capacity for Bifidin B2, while both of Bifidins B1 and B2 had almost close values for scavenging of superoxide anion radicals, 66 ± 1.970 % and 65.64 ± 1.343%, respectively. Bifidins demonstrated potential antitumor activity on two human cancer cell lines, MCF-7 and Skov-3, however, the antiproliferative activities does not exceed 60.8%. Bifidins B1 and B2 showed highest cytotoxicity against Skov-3 cells rather than MCF-7 cells, with IC50 values of 28.9± 8.76 µg/ml, and 29.87± 9.13 µg/ml, respectively.

Bioactive Phenolic Compounds from the Egyptian Red Sea Seagrass Thalassodendron ciliatum

2012 ◽  
Vol 67 (5-6) ◽  
pp. 291-296 ◽  
Author(s):  
Abdel-Hamid A. Hamdy ◽  
Walaa S. A. Mettwally ◽  
Mohamed Abou El Fotouh ◽  
Benjamin Rodriguez ◽  
Ahmed I. El-Dewany ◽  
...  
Keyword(s):  
Hepatitis A ◽  
Human Cancer ◽  
Racemic Mixture ◽  
Cytotoxic Activities ◽  
Human Cancer Cell Lines ◽  
Pure Compounds ◽  
Hct 116 ◽  
Thalassodendron Ciliatum ◽  
First Time ◽  
Mcf 7

Five flavonoids (rutin, asebotin, 3-hydroxyasebotin, quercetin-3-O-β-D-xylopyranoside, and a racemic mixture of catechin) and caffeic acid were isolated and identified for the first time from seagrass, Thalassodendron ciliatum, collected from the Hurghada region in Egypt. The crude extract and the isolated pure compounds were evaluated for their cytotoxic activities against HCT-116, HEPG, MCF-7, and HeLa human cancer cell lines, for their antiviral activity against Herpes Simplex and hepatitis A viruses, and for their antioxidant activity

scholarly journals CYTOTOXICITY OF FIVE PLANT EXTRACTS AGAINST DIFFERENT HUMAN CANCER CELL LINES AND THEIR MOLECULAR MECHANISM

2020 ◽  
pp. 194-198
Author(s):  
SALWA EL-HALLOUTY ◽  
ASHWAQ BATAWI ◽  
MANAL SHAFI ◽  
ESAM RASHWAN ◽  
EZZELDIN ELHAWARY ◽  
...  
Keyword(s):  
Cell Lines ◽  
Plant Extracts ◽  
Normal Cell ◽  
Human Cancer ◽  
Human Tumor ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Bax Gene ◽  
Mcf 7

Objective: Five methanol plant extracts namely, Euphorbia hierosolymitana, Dracaena marginata, Cordyline terminalis, and Sapium sebifera were screened in vitro for their cytotoxic effect on human tumor cell lines; namely, PC-3, HepG-2, HCT-116, and MCF-7 (prostate, liver, colon, and breast cancer) and human normal cell lines, namely, BJ-1. Methods: E. hierosolymitana (extract A) selectively inhibited HCT-116 cell proliferation with IC50 of 4.22 μg/ml, both Dracaena marginata (extract B) (bark, leaves, and branches) showed moderate cytotoxicity on MCF-7 with IC50 of 22.4 and 48.2 μg/ml, respectively. The remaining two extracts showed minimal to insignificant percentage inhibition on all cell lines. Results: E. hierosolymitana extract was selected for further studying, where the effect of the extract on the HCT116 cells showed a downregulation of her2 and Bcl-2 gene and overexpression of the Bax gene. Flow cytometry analysis was also performed to understand the effect of E. hierosolymitana on the apoptosis induction and the cell cycle. The results showed the induction of early and late apoptosis by 5.81 and 10.01%, respectively. Conclusion: Our results infer that E. hierosolymitana has a promising chance in fighting colorectal cancer due to its high cytotoxic effects on HCT116 cancer cells while having minimal effects on the BJ-1 normal cell lines.

scholarly journals Synthesis, Characterization, and Preliminary In Vitro Cytotoxic Evaluation of a Series of 2-Substituted Benzo [d] [1,3] Azoles

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2780
Author(s):  
Ozvaldo Linares-Anaya ◽  
Alcives Avila-Sorrosa ◽  
Francisco Díaz-Cedillo ◽  
Luis Ángel Gil-Ruiz ◽  
José Correa-Basurto ◽  
...  
Keyword(s):  
Binding Site ◽  
In Silico ◽  
Cytotoxic Effect ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Human Cancer Cell ◽  
Inhibitory Effects ◽  
Reference Drug ◽  
Human Cancer Cell Lines

A series of benzo [d] [1,3] azoles 2-substituted with benzyl- and allyl-sulfanyl groups were synthesized, and their cytotoxic activities were in vitro evaluated against a panel of six human cancer cell lines. The results showed that compounds BTA-1 and BMZ-2 have the best inhibitory effects, compound BMZ-2 being comparable in some cases with the reference drug tamoxifen and exhibiting a low cytotoxic effect against healthy cells. In silico molecular coupling studies at the tamoxifen binding site of ERα and GPER receptors revealed affinity and the possible mode of interaction of both compounds BTA-1 and BMZ-2.

Six New neo-Clerodane Diterpenoids from Aerial Parts of Scutellaria barbata and Their Cytotoxic Activities

Planta Medica ◽  
2018 ◽  
Vol 84 (17) ◽  
pp. 1292-1299 ◽  
Author(s):  
Guo-Chun Yang ◽  
Jia-Hui Hu ◽  
Bing-Long Li ◽  
Huan Liu ◽  
Jia-Yue Wang ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Cytotoxic Activities ◽  
Scutellaria Barbata ◽  
Human Cancer Cell Lines ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Clerodane Diterpenoids

AbstractSix new neo-clerodane diterpenoids (1–6), scutebatas X – Z, A1-C1, along with twelve known ones (7–18) were obtained via the phytochemical investigation of the aerial parts of Scutellaria barbata. Their structures were established by detailed spectroscopic analysis. The absolute configurations of 1 and 2, as the representative members of this type, were identified based on a circular dichroic exciton chirality method. Moreover, in vitro cytotoxicity of compounds 1–6 were evaluated against three human cancer cell lines (SGC-7901, MCF-7, and A-549) using the MTT method. Compound 6 showed cytotoxic activities against all the three cell lines with IC50 values of 17.9, 29.9, and 35.7 µM, respectively.

CYTOTOXIC ACTIVITY OF LUVUNGA SCANDENS AGAINST HUMAN CANCER CELL LINES

2016 ◽  
Vol 78 (10) ◽  
Author(s):  
Putri Nur Hidayah Al-Zikri ◽  
Muhammad Taher ◽  
Deny Susanti ◽  
Solachuddin Jauhari Arief Ichwan
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
A549 Cell ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Breast Adenocarcinoma ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.

Sign in / Sign up

Export Citation Format

Share Document