scholarly journals Synthesis of 1-[(Aryl)(3-amino-5-oxopyrazolidin-4-ylidene) methyl]-2-oxo-1,2-dihydroquinoline-3-carboxylic Acid Derivatives and Their Breast Anticancer Activity

Crystals ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 571
Author(s):  
Ahmed Gaber ◽  
Walaa F. Alsanie ◽  
Majid Alhomrani ◽  
Abdulhakeem S. Alamri ◽  
Ibrahim M. El-Deen ◽  
...  

This research aimed to produce new 1-[(aryl)(3-amino-5-oxopyrazolidin-4-ylidene) methyl]-2-oxo-1,2-dihydroquinoline-3-carboxylic acid derivatives and check their anticancer effect against the breast cancer MCF-7 cell line. The 2-oxo-1,2-dihydroquinoline-3-carboxylic acid (4) compound was obtained by hydrolyzing ethyl 2-oxo-1,2-dihydroquinoline-3-carboxylate (2) with thiourea and anhydrous potassium carbonate ethanol, which was then treated with ethyl 3-substituted 2-cyanoacrylates (6) in the presence of triethylamine in diethyl formamide to give 1-[2-(ethoxy)carbonyl-2-cyano-1-arylvinyl]-2-oxo-1,2-dihydroquinoline-3-carboxylic (7a,d). Cyclization of compound 7 with hydrazine hydrate ethanol inferred the association of 1-[(aryl)(3 amino-5-oxopyrazolidin-4-ylidene)methyl-2-oxo-1,2-dihydroquinol-3-carboxylates (8a,d). Spectroscopic and micro-analytical techniques such as IR, NMR, and elemental analysis were used to validate the structure of the synthesized organic compounds. The anticancer effects of the synthesized compounds 7a–d and 8a–d were tested by using the MTT assay on the MCF-7 cell line. When compared to the reference compound Dox, the compounds 7b, 7c, 8a, 8b, and 8c demonstrated strong anticancer activity against the MCF-7 cell line. The anticancer effects of the synthesized compounds 7a–d and 8a–d were tested against the MCF-7 cell line, using MTT assay. The compounds 7b, 7c, 8a, 8b, and 8c showed significant anticancer activity compared to the reference compound Dox against the MCF-7 cell line.

2021 ◽  
Author(s):  
Mohammad Mousavi-Khattat ◽  
Hamid Nourbakhshan ◽  
Mehrnaz Roumi ◽  
Mahshid Ebrahiminejad ◽  
Yasaman Fazeli ◽  
...  

Abstract Green synthesis methods are environmentally friendly, cost effective and nonhazardous for biomedical applications in comparison with other methods. The aim of the study was green synthesis of silver nanoparticles using medicinal animal dung extract as a reducing, capping and stabilizing agent for the first time among other synthesis methods of silver nanoparticles. Female donkey’s dung was capable to reduce silver ions to nanoparticles and stabilize them. Silver nanoparticles with average sizes of 36 nm were synthesized and characterized by UV-Vis, FT-IR, XRD and TEM. Moreover, synthesized nanoparticles were analyzed in terms of anticancer activity by MTT assay on MCF-7 cell line. UV–Visible spectrophotometer showed an absorbance peak in the range of 414-433 nm. To identify the phytochemical coating of particles, FTIR analysis was used. Transmission electron microscope (TEM) images and X-ray diffraction (XRD) confirmed the formation of small spherical silver nanoparticles. The MTT assay revealed potent anticancer effects of the aqueous extract synthesized nanoparticles on MCF-7 cells, incubated for 24 hours. Based on the current findings, it is strongly believing that the use of donkey’s dung offers large scale production of biocompatible silver nanoparticles that can be suggested to possess valuable anticancer agents against breast cancer cell lines.


2019 ◽  
Vol 7 (22) ◽  
pp. 3904-3906
Author(s):  
Delisma Simorangkir ◽  
Masfria Masfria ◽  
Urip Harahap ◽  
Denny Satria

BACKGROUND: Cancer is one of the causes of morbidity and mortality worldwide. Breast cancer is one of the most common types of cancer in Indonesia. Failures that often occur in the treatment of cancer primarily through chemotherapy, synthetic drugs that have side effects include anemia, alopecia, cardiotoxic and hepatotoxic due to low anti-cancer selectivity and unclear carcinogenesis process. Cyperus rotundus L. rhizome is one of the medicinal plants that potential enough to be developed as an anticancer agent. AIM: The aim of this study was to anticancer activity n-hexane fraction Cyperus rotundus L. rhizomes to breast cancer MCF-7 cell line in vitro. METHODS: Cyperus rutundus L. rhizomes powder was extracted ethanol by percolation then fractionated with n-hexane. Phytochemical screening was then carried out. The cytotoxic activity of the n-hexane fraction was determined by observing this extract on MCF-7 cells using the (3- (4,5-dimethylimidazole-2-il) -2,5-diphenyl tetrazolium bromide) (MTT). Selectivity index (IS) of normal cells (Vero cells). Cell cycle and apoptosis induction were analyzed by flow cytometry. RESULTS: The result showed that the fraction n-hexane Cyperus rutundus L. rhizome has anticancer activity against breast cancer MCF-7 cells with accumulation cell cycle in the G0-G1 phase and through induction of apoptosis. CONCLUSION: The n-hexane fraction Cyperus rotundus L. rhizome has potent anticancer activity.


Author(s):  
Debarshi Kar Mahapatra ◽  
Devashish Das ◽  
Ruchi Shivhare

Cancer is the second leading causes of mortality across the planet which has had affected millions. In spite of massive efforts in producing new molecules and chemotherapeutic approaches for managing cancer, it continued to be the global threat. Small hybrid molecules have gained popularity in chemotherapy due to their potential and smart characteristics in modulating biological targets. The present research attempts in developing few novel hybridized derivatives of murrayanine (an active carbazole derivative) by the semi-synthetic approach to form substituted thiazole linked murrayanine-Schiffs base derivatives. The protocol involved murrayanine 1 as the template material for constructing a hybridized Schiffs base intermediate 3, which further by Hantzchs cyclization was subsequently converted to various hybridized thiazoles analogs 5a-5f. The purity of the synthesized compounds was ascertained by sophisticated analytical techniques. The anti-cancer potential was screened against breast cancer cell lines; MCF-7 and MDA-MB-231 by Sulforhodamine B (SRB) assay. The compound 5b displayed most potent anti-proliferative activity with IC50 values of 23.41?M against MCF-7 cell line and 32.15?M against MDA-MB-231 cell line. It has been observed that analogs having electron withdrawing substituents exhibited pronounced anticancer activity. The docking study was performed by Autodock Vina where the results were found to be in full agreement with the cytotoxic study, depicting that the probable cytotoxic outcome by EGFR inhibitory mechanism. The study revealed the potential of novel hybridized derivatives as active anti-breast cancer candidates. The research will encourage (medicinal) chemists in rationally designing of semi-synthetic analogs of a heterocyclic prototype having pronounced anti-cancer activity.


Author(s):  
S. Vijayakumar ◽  
V. Bhuvaneshwari ◽  
A. Sumathi

Breast cancer is one of the major health problems among women in both developed and developing countries. The objective of the present investigation is focused on the DPPH Radical Scavenging Activity and anticancer effect of the methanolic extract of Moringa concanensis Nimmo leaves against Breast cancer (MCF-7) cell line. The study was facilitated by collecting the plant sample and subjected to crude extraction. The anticancer activity of the crude methanolic leaf extract of M. concanensis against MCF- 7 cell line was examined by MTT assay. The present study confirms that the crude leaf extract of M. concanensis has potential anticancer activity against MCF- 7 cell lines while compared to the control. M. concanensis leaves possess remarkable anticancer property which may lead to development of novel compounds as natural phytomedicine.


Author(s):  
Rajesh Shah

Background Cancer is one of the leading causes of mortality. The recent experiments with high-diluted preparations have shown anticancer effects in in-vitro and vivo models. The fundamental principle of homeopathy suggests that the substances capable of producing certain diseases may have a capacity to alter the same disease if used in the ultra-dilute-potentized form. This hypothesis led certain carcinogens for examining their potential anti-cancer efficacy. Method Sulforhodamine B assay is useful in determining the cytotoxicity in cell-based studies in evaluating anticancer agents. The protocol involved preparation of homeopathy dilutions, incubation of cells with homeopathy dilutions, SRB binding, and measurement of absorbance. Cells were treated with 30 potencies of HIV nosode, Hepatitis C nosode, Carcinosin, Cancer nosode, and Ethanol along with positive control (Adriamycin). The preparations were tested in HeLa, HepG2, A549, MCF 7, T 24, Jurkat, SCC 40, and HL-60 cell-lines. Results The homeopathic preparations have shown the anticancer activity measured as percentage growth inhibition. All the homeopathy preparations studied, exhibited anticancer activity on HeLa, HepG2, A 549, T 24, and HL-60 cells. Carcinosin showed the anticancer activity on the SCC 40 cells. Hepatitis C nosode, Carcinosin, and Cancer nosode have shown the anticancer activity on breast cancer cell line MCF-7. None of the preparations exhibited anticancer activity on Human Leukemia Cell Line. Conclusion High-dilution, potentized preparations of certain carcinogens have demonstrated anti-cancer, cytotoxic effects in the cell-line model, supporting the rationale of the fundamental homeopathic principle the Law of Similars, opening windows to its wider applications in healthcare.


2020 ◽  
Vol 10 (6) ◽  
pp. 806-816
Author(s):  
Sabiha Zamani ◽  
Danish Idrees ◽  
Babita Jha ◽  
Anal K. Jha

Background:: At the present time, silver and gold nanoparticles are emerging as promising agents for cancer therapy. The anticancer activities of these nanoparticles have been evaluated against numerous human cancer cell lines. Still, few reports were existing against the breast cancer cell lines and most of these studies have mainly used chemically mediated nanoparticles. Objective:: This study reports the in vitro anticancer activity of bioinspired Nanoparticles like, silver and gold against MCF-7 cells (breast cancer cell line) as well as HEK293 cell (human embryonic kidney cell line) by MTT assay. Methods: These metal nanoparticles, Ag-NPs and Au-NPs were biologically synthesized using Adiantum sp. aqueous leaves extract. The Adiantum sp. can reduce HAuCl4 solution to Au-NPs and AgNO3 to Ag-NPs within 30 mins. The formation of NPs was confirmed by characterization techniques such as UV-vis spectrophotometer, SEM and XRD studies. Additionally, the anticancer activity was analysed by cell viability (3(4,5-dimethly-thiazol-2-yl)- 2,5-diphenyl tetrazo-lium bromide assay). Results: The synthesized nanoparticles from Adiantum sp. were characterized by UV-visible spectroscopy. The role of functional groups was analysed using a Fourier Transform Infrared (FTIR) spectrophotometer. The XRD pattern clearly exemplified that the nanoparticles formed in this present synthesis are crystalline in nature. Furthermore, in MTT assay study, both NPs have shown cytotoxicity at different concentrations ranging from 2.5 to 100 μg/ml. The data reveal that the NPs from Adiantum explicitly, inhibits the viability of cancerous cell only and are non-cytotoxic to HEK293 cells in the tested concentration range. Conclusion: The results provide a preliminary guidance that Adiantum mediated silver and gold nanoparticles might be used to treat breast cancer; however, it necessitates clinical studies to ascertain their potential as anticancer agents.


Sign in / Sign up

Export Citation Format

Share Document