scholarly journals Synthesis, Structure, Electrochemistry, and Cytotoxic Properties of Ferrocenyl Ester Derivatives

2009 ◽  
Vol 2009 ◽  
pp. 1-8 ◽  
Author(s):  
Li Ming Gao ◽  
Ramón Hernández ◽  
Jaime Matta ◽  
Enrique Meléndez
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
State Structure ◽  
X Ray ◽  
X Ray Crystallography ◽  
Viability Assay ◽  
Cyclopentadienyl Ligand ◽  
Ht 29 ◽  
Lipophilic Character ◽  
Mcf 7

A series of ferrocenyl ester complexes, varying the lipophilic character of the pendant groups, was prepared and characterized by spectroscopic and analytical methods. The syntheses of Fe(C5H4CO2CH3)2, Fe(CpCOOCH3) (CpCOO CH2CH3), and Fe(CpCOOCH2CH3)2 are reported. The solid-state structure of Fe(C5H4CO2CH3)2 has been determined by X-ray crystallography. Fe(C5H4CO2CH3)2 has the cyclopentadienyl rings virtually in an eclipsed conformation with the pendant groups not completely opposite to each other. Cyclic voltammetry characterization showed that the functionalized ferrocenes oxidize at potentials, Epa, higher than ferrocene as a result of the electro withdrawing effect of the pendant groups on the cyclopentadienyl ligand. The cytotoxicities of Fe(C5H4CO2CH2CH2OH)2, Fe(C5H4CO2CH2CH=CH2)2, Fe(C5H4CO2CH3)2, Fe(CpCOOCH3)(CpCOOCH2CH3), and Fe(CpCOOCH2CH3)2 in colon cancer HT-29 and breast cancer MCF-7 cell lines were measured by the MTT biological viability assay and compared to ferrocene and ferrocenium. Fe(C5H4CO2CH2CH=CH2)2 showed the best IC50 values, 180(10)  μM for HT-29 and 190(30)  μM for MCF-7 cell lines, with cytotoxicities similar to ferrocenium. The cytotoxic data suggest that as we increase the lipophilic character of the functionalized ferrocene, the cytotoxicity improves approaching to the cytotoxic activity of ferrocenium.

scholarly journals New Amides and Phosphoramidates Containing Selenium: Studies on Their Cytotoxicity and Antioxidant Activities in Breast Cancer

Antioxidants ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 590
Author(s):  
Mikel Etxebeste-Mitxeltorena ◽  
Daniel Plano ◽  
Nora Astrain-Redín ◽  
Cristina Morán-Serradilla ◽  
Carlos Aydillo ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Death ◽  
Cell Lines ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Cycle Arrest ◽  
Ht 29 ◽  
Mcf 7 ◽  
Nonmalignant Cell

Breast cancer is a multifactor disease, and many drug combination therapies are applied for its treatment. Selenium derivatives represent a promising potential anti-breast cancer treatment. This study reports the cytotoxic activity of forty-one amides and phosphoramidates containing selenium against five cancer cell lines (MCF-7, CCRF-CEM, HT-29, HTB-54 and PC-3) and two nonmalignant cell lines (184B5 and BEAS-2B). MCF-7 cells were the most sensitive and the selenoamides I.1f and I.2f and the selenium phosphoramidate II.2d, with GI50 values ranging from 0.08 to 0.93 µM, were chosen for further studies. Additionally, radical scavenging activity for all the compounds was determined using DPPH and ABTS colorimetric assays. Phosphoramidates turned out to be inactive as radical scavengers. No correlation was observed for the antioxidant activity and the cytotoxic effect, except for compounds I.1e and I.2f, which showed dual antioxidant and antitumor activity. The type of programmed cell death and cell cycle arrest were determined, and the results provided evidence that I.1f and I.2f induced cell death via autophagy, while the derivative II.2d provoked apoptosis. In addition, Western blot analysis corroborated these mechanisms with an increase in Beclin1 and LC3-IIB and reduced SQSTM1/p62 levels for I.1f and I.2f, as well as an increase in BAX, p21 and p53 accompanied by a decrease in BCL-2 levels for derivative II.2d.

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 Unexpected Synthesis, Single-Crystal X-ray Structure, Anticancer Activity, and Molecular Docking Studies of Certain 2–((Imidazole/Benzimidazol–2–yl)thio)–1–arylethanones

Crystals ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 446
Author(s):  
Tarfah Al-Warhi ◽  
Mohamed Said ◽  
Mahmoud El Hassab ◽  
Nada Aljaeed ◽  
Hazem Ghabour ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Molecular Docking ◽  
Single Crystal ◽  
Cell Lines ◽  
Docking Study ◽  
Anticancer Activities ◽  
Molecular Docking Study ◽  
X Ray ◽  
Mcf 7

In connection with our research program concerning development of novel effective benzimidazole-based anticancer candidates, herein we describe a new unexpected synthetic route to obtain a series of 2–((imidazole/benzimidazol2–yl)thio)1–arylethanones endowed with promising anti-breast cancer and Cyclin-dependent kinase 2 (CDK2) inhibitory activities. Contrary to expectations, products for the reaction of 2–mercaptoimidazole/benzimidazole 2a,b with β–keto esters 6a–c were unambiguously assigned as 2–((imidazol/benzimidazol2–yl)thio)1–arylethanones 10a–f based on NMR spectroscopy and single-crystal X-ray crystallographic analyses. In vitro anticancer activities for herein reported imidazole/benzimidazoles 10a–f were assessed through a cell-based assay against human breast cancer T4–7D and MCF–7 cell lines. Benzimidazoles 10d–f exerted better anti-proliferative action towards T4–7D and MCF–7 cell lines than their corresponding imidazole counterparts 10a–c. Furthermore, a molecular docking study suggested CDK2 kinase as a potential enzymatic target for benzimidazoles 10d–f, and investigated their possible binding pattern and interactions within CDK2 active site. Thereafter, benzimidazoles 10d–f were in vitro examined for their CDK2 inhibitory action, where they exerted good activity. Finally, several key ADME and druglikeness properties were predicted by the SwissADME online tool. Interestingly, benzimidazoles 10d–f were found to have no violations in all druglikeness rules (Veber, Lipinski, Ghose, Muegge, and Egan). In addition, they had neither PAINS nor structural alerts (Brenks). In conclusion, benzimidazoles 10d–f demonstrated not only a promising anticancer activities but also an acceptable ADME and physicochemical properties especially benzimidazole 10e.

scholarly journals ROS Reduction Does Not Decrease the Anticancer Efficacy of X-Ray in Two Breast Cancer Cell Lines

2019 ◽  
Vol 2019 ◽  
pp. 1-12 ◽  
Author(s):  
Huizhen Wang ◽  
Xin Zhang
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
X Rays ◽  
Anticancer Efficacy ◽  
X Ray ◽  
Mcf 7

Radiotherapy is effective on a large number of cancer types and is one of the most frequently administrated treatments for cancer patients. The anticancer efficacy of X-ray radiotherapy has been frequently correlated with reactive oxygen species (ROS) elevation, which is also a limiting factor for its toxicity on normal tissues. Here, we found that although 4-10 Gy X-rays could significantly reduce cell numbers in both MDA-MB-231 and MCF-7 breast cancer cells, the ROS level changes are less in MCF-7 cells than in MDA-MB-231 cells. Moreover, although both the ROS scavenger N-acetyl-L-cysteine (NAC) and 1 T static magnetic field (SMF) could reduce X-ray-induced ROS elevation, they did not prevent X-ray-induced cell number reduction or cell death increase, which is significantly different from cisplatin. These results demonstrate that although the anticancer efficacy of cisplatin on two breast cancer cell lines is dependent on ROS, the anticancer efficacy of X-ray is not. Moreover, by testing 19 different cell lines, we found that 1 T SMF could effectively reduce ROS levels in multiple cell lines by 10-20%, which encourages further studies to investigate whether SMF could be used as a potential “physical antioxidant” in the future.

scholarly journals ANTICANCER ACTIVITY OF CAMELLIA SINENSIS MEDIATED COPPER NANOPARTICLES AGAINST HT-29, MCF-7 AND MOLT-4 HUMAN CANCER CELL LINES

2017 ◽  
Vol 10 (2) ◽  
pp. 82 ◽  
Author(s):  
Vijay D. Mendhulkar ◽  
Anu Yadav
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Camellia Sinensis ◽  
Copper Nanoparticles ◽  
Cancer Cell Lines ◽  
Leukemia Cell Line ◽  
Synergistic Activity ◽  
Ht 29 ◽  
Mcf 7

Objective: With the advancement in nanotechnology, it is imperative to unearth its applications in medicine. Present investigation deals with the copper nanoparticles biosynthesizing capability of the leaves of medicinally important plant, Camellia sinensis.Methods: The phytosynthesized CuNPs were characterized by EDX, NTA, XRD, SEM, TEM and FTIR analysis. In the current study, we have made attempts to exploit the anticancer ability of the copper nanoparticles against HT-29 colon cancer, MCF 7 breast cancer and MOLT-4 leukemia cancer cell lines via SRB assay. We also carried out the synergistic activity with standard drug Adriamycin (ADR).Results: The synthesis of CuNPs was confirmed using EDX analysis where the presence of a strong optical absorption peak was observed at 1 keV, which is typical for the absorption of metallic copper nanoparticles. According to the results obtained, CuNPs showed good antiproliferative results in a dose dependant manner on HT-29 and MCF-7 cell lines, with 80 µg/ml concentration giving the best result. The synergistic effect of CuNPs+ADR was even better than that of CuNPs alone on all the cell lines. The synergism drug combinations showed highly responsive results on the leukemia cell line compared to individual drugs.Conclusion: Among all the treatments and cell lines studied, the most favorable and responsive antiproliferative impact was recorded for CuNPs+ADR combination treatment at 40µg/ml concentration on MCF-7 breast cancer cell line.Keywords: CuNPs, Camellia sinensis, Anticancer, Sulforhodamine B assay, HT-29, MCF-7, MOLT-4.

Synthesis and Antitumor Activity of Some N2-(Thien-3-yl)amidrazones

2014 ◽  
Vol 69 (7) ◽  
pp. 811-816 ◽  
Author(s):  
Mohammed M. Abadleh ◽  
Mustafa M. El-Abadelah ◽  
Salim S. Sabri ◽  
Hanan H. Mohammed ◽  
Malek A. Zihlif ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Antitumor Activity ◽  
Cell Viability ◽  
Cell Lines ◽  
K562 Cell ◽  
Cyclic Amine ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
A Cell ◽  
Mcf 7

6aA set of new N2-(thien-3-yl)amidrazones (-h) incorporating N-piperazines and related congeners has been synthesized by reacting the hydrazonoyl chloride 4(derived from 3-aminothiophene- 2-carboxylate) with the appropriate sec-cyclic amine. The antitumor activity of these compounds was evaluated on breast cancer (MCF-7) and leukemic (K562) cell lines by a cell viability assay utilizing the tetrazolium dye (MTT). The amidrazone 6d encompassing the N-piperazine moiety, was the most active against MCF-7 and K562 with IC50 of 7.28 and 9:91 μM, respectively.

scholarly journals Synthesis, X-Ray Crystal Structures, and Preliminary Antiproliferative Activities of New s-Triazine-hydroxybenzylidene Hydrazone Derivatives

2019 ◽  
Vol 2019 ◽  
pp. 1-10 ◽  
Author(s):  
Assem Barakat ◽  
Fardous F. El-Senduny ◽  
Zainab Almarhoon ◽  
Hessa H. Al-Rasheed ◽  
Farid A. Badria ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Hydroxyl Group ◽  
X Ray ◽  
Synthetic Strategy ◽  
Weak Activity ◽  
Hct 116 ◽  
Antiproliferative Activities ◽  
Mcf 7

We herein report a new small library of Schiff-base compounds that encompasses s-triazine and (2 or 4)-hydroxylbenzylidene derivatives. These compounds were synthesized through a hydrazone linkage connecting both the s-triazine and hydroxybenzylidene derivatives. The synthetic strategy adopted allowed the synthesis of the target compounds with excellent yields and purities as observed from their NMR (1H and 13C) and elemental analysis. Furthermore, 4f, 5b, and 5f were further confirmed by X-ray single crystal diffraction technique. The preliminary antiproliferative activities for the synthesized compounds were tested against two different cancer cell lines including breast cancer (MCF-7) and colon cancer (HCT-116). From the eighteen compounds, which have been examined, only two derivatives having piperidine moiety showed more selectivity against the two cell lines MCF-7 and HCT-116, while the others showed very weak activity. The position of the hydroxyl group in the benzylidine ring and the substituent on the s-triazine moiety has great effect on the activity of the prepared compounds. The IC50 values for the two derivatives 4a and 5a evaluated against breast cancer cells, very close to those for the chemotherapeutic drug cisplatin, are 27 µM (13.3 µg/mL), 17 µM (8.4 µg/mL), and 20 µM (6 µg/mL) for 4a, 5a, and cisplatin, respectively. These results propose the preliminary antiproliferative activity of these two derivatives may deserve further consideration for development of new derivatives as potent anticancer agents.

scholarly journals APRICOXIB

2018 ◽  
Vol 25 (12) ◽  
pp. 1915-1922
Author(s):  
Fatima Rizvi ◽  
Syed Mahboob Alam ◽  
Farah Asad ◽  
Hina Shams
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Mtt Assay ◽  
Cytotoxic Effects ◽  
Inflammatory Conditions ◽  
Ic50 Value ◽  
Ht 29 ◽  
Mcf 7

Background: Breast cancer is most frequently diagnosed cancer globally but there is not any ideal economical and safer agent that not only decreases the progression but also resolve complexities associated with breast cancer such as inflammatory conditions. There was strong link between inflammation and cancer specially breast cancer. Thus by inhibiting the COX enzyme may inhibit the progression of cancer beside of its role in inflammatory conditions of breast. Study Design: Interventional In Vitro trial. Setting: Department of Pharmacology in alliance with PCMD. Period: The duration of study from April 2016 to February 2017. Methodology: For this purpose we used five cancerous lines MCF-7, MDA-MB-231, MCF-10, HT-29 and Hela cell lines. For demonstrating the cytotoxic effects of Apricoxib we used MTT assay (for all cell Lines) and Trypan blue dye exclusion assay (Primarily for MCF-7 cell lines). For calculation of minimum dose required for exert cytotoxic effects of Apricoxib and its selectivitytowards cancerous cells of breast tissue we calculated its IC50 value and Selectivity Index (SI) by MTT assay. Results: Apricoxib significantly reduce the viability of MCF-7, MDA-MB-231, Hela, HT-29 as assessed by MTT assay in dose dependent manner (χ2 (2) = 26.483, p<0.001), (χ2 (2) = 26.49, p<0.001), (χ2 (2) = 26.062, p<0.001) and (χ2 (2) = 26.062, p<0.001) respectively. However Apricoxib had non-significant effects on % viability of MCF-10 cell line (χ2 (2) = 4.167, p=0.654) as assessed by MTT assay. Furthermore Apricoxib had lowest IC50 value against MCF-7 cell line. Conclusion: This study demonstrated that beside of primarily anti-inflammatory effects Apricoxib have additional benefits in term of exerting the cytotoxic effects (in vitro) on cancerous cell lines as indicated by reducing the % viability and reducing the Absorbance value of test sample as compare to control. This opens the newer path for researcher to evaluate different aspects of Apricoxib in field of chemotherapy.

scholarly journals HPLC-DAD-Guided Isolation of Diversified Chaetoglobosins from the Coral-Associated Fungus Chaetomium globosum C2F17

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1237 ◽  
Author(s):  
Xiao-Wei Luo ◽  
Cheng-Hai Gao ◽  
Hu-Mu Lu ◽  
Jia-Min Wang ◽  
Zi-Qi Su ◽  
...  
Keyword(s):  
Single Crystal ◽  
Cell Lines ◽  
Cancer Cell ◽  
Spectroscopic Analysis ◽  
Chaetomium Globosum ◽  
X Ray ◽  
X Ray Crystallography ◽  
Ic50 Values ◽  
First Time ◽  
Mcf 7

Cytochalasans have continuously aroused considerable attention among the chemistry and pharmacology communities due to their structural complexities and pharmacological significances. Sixteen structurally diverse chaetoglobosins, 10-(indol-3-yl)-[13]cytochalasans, including a new one, 6-O-methyl-chaetoglobosin Q (1), were isolated from the coral-associated fungus Chaetomium globosum C2F17. Their structures were accomplished by extensive spectroscopic analysis combined with single-crystal X-ray crystallography and ECD calculations. Meanwhile, the structures and absolute configurations of the previously reported compounds 6, 12, and 13 were confirmed by single-crystal X-ray analysis for the first time. Chaetoglobosins E (6) and Fex (11) showed significant cytotoxicity against a panel of cancer cell lines, K562, A549, Huh7, H1975, MCF-7, U937, BGC823, HL60, Hela, and MOLT-4, with the IC50 values ranging from 1.4 μM to 9.2 μM.

Cytotoxic activity and anti-cancer potential of Ontario grown onion extracts against breast cancer cell lines

2018 ◽  
Vol 8 (3) ◽  
pp. 159 ◽  
Author(s):  
Meghan Fragis ◽  
Abdulmonem I. Murayyan ◽  
Suresh Neethirajan
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Cancer Line ◽  
Mcf 7

Background: Breast cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths among Canadian women. Cancer management through changes in lifestyle, such as increased intake of foods rich in dietary flavonoids, have been shown to decrease the risk associated with breast, liver, colorectal, and upper-digestive cancers in epidemiologic studies. Onions are high in flavonoid content and one of the most common vegetables. Additionally, onions are used in most Canadian cuisines.Methods: We investigated the effect of five prominent Ontario grown onion (Stanley, Ruby Ring, LaSalle, Fortress, and Safrane) extracts on two subtypes of breast cancer cell lines: a triple negative breast cancer line MDA-MB-231 and an ER+ breast cancer line MCF-7.Results: These onion extracts elicited strong anti-proliferative, anti-migratory, and cytotoxic activities on both the cancer cell lines. Flavonoids present in these onion extracts induced apoptosis, cell cycle arrest in the G2/M phase, and a reduction in mitochondrial membrane potential at dose-dependent concentrations. Onion extracts were more effective against MDA-MB-231 compared to the MCF-7 cell line. Conclusion: In this study, we investigated the extracts synthesized from Ontario-grown onion varieties in inducing anti-migratory, cytostatic, and cytotoxic activities in two sub-types of human breast cancer cell lines. Anti-tumor activity of these extracts depends upon the varietal and can be formulated into nutraceuticals and functional foods for the wellbeing of cancer patients. Overall, the results suggest that onion extracts are a good source of flavonoids with anti-cancerous properties.Keywords: onion extracts; flavonoids; anti-proliferative; breast cancer; cytotoxic activity

Sign in / Sign up

Export Citation Format

Share Document