scholarly journals Synthesis and Characterization of Some New Coumarin Derivatives as Probable Breast Anticancer MCF-7 Drugs

Crystals ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 565
Author(s):  
Ahmed Gaber ◽  
Walaa F. Alsanie ◽  
Majid Alhomrani ◽  
Abdulhakeem S. Alamri ◽  
Ibrahim M. El-Deen ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Carboxylic Acids ◽  
Diethyl Malonate ◽  
Cancer Drug ◽  
Flow Cytometric ◽  
Anti Cancer ◽  
Elemental Analyses ◽  
M Phase ◽  
Mcf 7 ◽  
Phenyl Vinyl

This study aimed to synthesize quinolinone derivatives and investigate their cytotoxic activity. The compound 1-azacoumarin-3-carboxylic acid (2-oxo-1H-quinoline-3-carboxylic acid) was obtained via the cyclocondensation of 2-hydroxybenzaldehyde with diethyl malonate in base catalyst to give ethyl coumarin-3-carboxylate, followed by the ammonolysis of ester (ethyl coumarin-3-carboxylate) with ammonia in the presence of anhydrous potassium carbonate. Treatment of 2-oxo-1H-quinoline-3-carboxylic acid with acetic anhydride, cinnamaldehyde, cinnamic acid and methyl 5-phenyl-2-cyano-2,4-pentadienoate under different conditions led to the formation of 1 (substituted) aza coumarin-3-carboxylic acids (1-N-(acetyl)-azacoumarin-3-carboxylic acid 1-N-(2-Formyl-1-phenyl) vinyl-azacoumarin-3-carboxylic acids 1-N-[2-(Hydroxy) carbonyl-1-(Phenyl) vinyl]-azacoumarin-3-carboxylic acid and 1-N-(4-Cyano-5-methoxy-5-oxo-1-Phenylpenta-1,3-diene-1-y)-azacoumarin-3-carboxylic 284 acid), respectively. The structures of synthesized 1-(substituted) azacoumarin-3-carboxylic acids were confirmed based on spectroscopic methods (IR and NMR), along with elemental analyses. Interestingly compound 6 demonstrated probable impacts as an anti-cancer drug against the MCF-7 cell line. The mechanism of action was assessed using a flow cytometric assay. The outcomes revealed that compound 6 could arrest the cell cycle at G2/M phase and pre-G1 apoptosis.

Synthesis and anticancer evaluation of some coumarin and azacoumarin derivatives

2021 ◽  
Vol 23 (2) ◽  
pp. 27-34
Author(s):  
Safyah B. Bakare
Keyword(s):  
Carboxylic Acid ◽  
Elemental Analysis ◽  
Biological System ◽  
Analysis Data ◽  
Elemental Analysis Data ◽  
Coumarin Derivatives ◽  
Anti Cancer ◽  
Analgesic Agents ◽  
Mcf 7

Abstract Coumarin and its nitrogen analogue 1-aza coumarin are a class of lactones and lactams, respectively, which are indispensable heterocyclic units to both chemists and biochemists. 1-Aza coumarin derivatives, which ultimately metabolize as the corresponding 8-hydroxy coumarins in the biological system are therefore found to be very good anti-inflammatory, anti-cancer, and analgesic agents. A series of hybrid substituted coumarin and azacoumarin-3-carboxylic acid derivatives (8-methoxycoumarin-3-carboxylic acid (4a), 8-methoxyazacoumarin-3-carboxylic acid (4b), 5-bromo-8-methoxycoumarin-3-carboxylic acid (5a), 5-bromo-8-methoxyazacoumarin-3-carboxylic acid (5b), 2-acetoxy-5-bromo-8-methoxyquinoline-3-carboxylic acid (6), and 5,7-di(phenylazo)-8-methoxycoumarin-3-carboxylic acid (7) were synthesized and structurally proved using spectral and elemental analysis data. Substituted coumarin-3-carboxylic acid (4a and 5a) and Substituted azacoumarin-3-carboxylic acid (4b, 5b and 6) were tested for their in vitro cytotoxic activity against MCF-7 and HepG-2 cell lines.

scholarly journals Hydrophilic Polyhedral Oligomeric Silsesquioxane, POSS(OH)32, as a Complexing Nanocarrier for Doxorubicin and Daunorubicin

Materials ◽  
2020 ◽  
Vol 13 (23) ◽  
pp. 5512 ◽  
Author(s):  
Kinga Piorecka ◽  
Anna Janaszewska ◽  
Marta Majkowska ◽  
Monika Marcinkowska ◽  
Jan Kurjata ◽  
...  
Keyword(s):  
Drug Carrier ◽  
Correlation Spectroscopy ◽  
Hydroxyl Group ◽  
Cancer Drug ◽  
Breast Adenocarcinoma ◽  
Hydroxyl Groups ◽  
Polyhedral Oligomeric Silsesquioxanes ◽  
Molar Ratios ◽  
Anti Cancer ◽  
Mcf 7

A novel strategy, recently developed by us, to use polyhedral oligomeric silsesquioxanes (POSS) as an anti-cancer drug carrier is presented. Anthracycline:POSS complexes were prepared by simple co-addition of doxorubicin (DOX) or daunorubicin (DAU) with hydrophilic POSS(OH)32. Co-delivery of POSS and anthracyclines led to higher anti-cancer activity towards HeLa (cervical cancer endothelial) and MCF-7 (human breast adenocarcinoma) cell lines. The obtained supramolecular hybrid complexes were characterised by nuclear magnetic resonance (NMR) spectroscopy (nuclear Overhauser effect spectroscopy [NOESY] and homonuclear correlation spectroscopy [COSY]), Fourier transform infrared spectroscopy (FTIR), and dynamic light scattering (DLS). The two-dimensional (2D) NOESY spectra of the complexes showed the cross-correlation peaks for hydroxyl groups of POSS (~4.3–4.8 ppm) with OH groups of DOX and DAU. FTIR showed that hydroxyl group of POSS can interact with amine and hydroxyl groups of DOX and DAU. The viability of HeLa and MCF-7 was analysed with the MTT assay to evaluate the cytotoxicity of free DOX and DAU and the relevant complexes with POSS at different molar ratios. At a low DOX concentration (2.5 µM), for molar ratios 1:1, 1:4, and 1:8 (POSS:DOX), the complexes showed two and three times higher cytotoxicity towards HeLa and MCF-7 cells, respectively, than DOX itself after both 24- and 48-h incubation. The 1 µM concentration for a 1:4 POSS:DOX molecular ratio and the 2.5 µM concentration for all complexes were more toxic towards MCF-7 cells than free DOX after 48-h incubation. In the case of POSS:DAU complexes, there was higher toxicity than that of free drug after 48-h incubation. It can be concluded that the formation of non-covalent complexes increases toxicity of anthracycline drugs towards Hela and MCF-7 cells. The novel complexes are inexpensive to prepare and more effective than free drugs at low systemic toxicity.

Synthesis, spectral, molecular modeling, biological and antitumor studies of new nifuroxazide complexes

2021 ◽  
Vol 11 (7) ◽  
pp. 1071-1083
Author(s):  
Eid H. Alosaimi ◽  
Walaa H. El-Shwiniy ◽  
Saad M. Alshahrani ◽  
Ayman A. O. Younes ◽  
Mostafa Y. Nassar ◽  
...  
Keyword(s):  
Bacterial Species ◽  
Thermal Analyses ◽  
Molar Conductance ◽  
Cancer Drug ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Anti Cancer ◽  
Hct 116 ◽  
Mcf 7

Series of Zr(IV), Ce(IV) and U(VI) complexes were synthesized with nifuroxazide ligand. Design and formulae of the complexes suggested in the light of analytical, spectral, magnetic and thermal analyses (1HNMR, IR, UV-Vis). The calculated values of molar conductance mean that, all isolated complexes were electrolytes. The data revealed the complexes formation and suggested that nifuroxazide binds as a bidentate at NO sites with metal ions. The kinetic parameters evaluated using Coats Redfern (CR) and Horowitz-Metzeger (HM) methods. The thermodynamic data reflect the thermal stability for all complexes. The calculated bond length and force constant values for UO2 bond are 1.741 Å and 459.409 Nm−1. The research investigations were related to quantum chemical calculations conducted at the theory level of DFT/B3LYP/LANL2DZ. The nifuroxazide, inorganic salts and their metal complexes were assayed against different bacterial species as well as the in vitro growth inhibitory activity against human breast carcinoma (MCF-7) and HCT-116 cell lines. Zr(IV) complex was found to have the highest activity against all the tested organisms and a powerful anti-cancer drug.

scholarly journals Anticancer activity of some new series of 2-(substituted)amino-1,3-thiazole derivatives

2019 ◽  
Vol 21 (3) ◽  
pp. 19-25
Author(s):  
Safyah B. Bakare
Keyword(s):  
Caspase 3 ◽  
Flow Cytometric Assay ◽  
Thiazole Derivatives ◽  
H Nmr ◽  
Cycle Arrest ◽  
Flow Cytometric ◽  
Elemental Analyses ◽  
M Phase ◽  
Line Compound ◽  
C Nmr

Abstract A series of thiazole derivatives were synthesized and structurally elucidated by IR, 1H NMR, 13C NMR, mass and elemental analyses. The prepared compounds were screened for their cytotoxic activity against Leukemia HL-60 cell line. Compound 4b was considered as the most promising antitumor candidate among the tested compounds. Mechanism of action of compound 4b evaluated by flow cytometric assay revealed cell cycle arrest at G2/M phase and pre-G1 apoptosis. The ratio of apoptosis was also determined. Moreover, compound 4b increased the concentration of caspase 3 by 4 fold more than untreated control.

Poly-carboxylic acids functionalized chitosan nanocarriers for controlled and targeted anti-cancer drug delivery

2016 ◽  
Vol 83 ◽  
pp. 201-211 ◽  
Author(s):  
Mariappan Rajan ◽  
Maruthamuthu Murugan ◽  
Deepalekshmi Ponnamma ◽  
Kishor Kumar Sadasivuni ◽  
Murugan A. Munusamy
Keyword(s):  
Drug Delivery ◽  
Carboxylic Acids ◽  
Cancer Drug ◽  
Anti Cancer ◽  
Cancer Drug Delivery

Boron Spirochelates Derived from Some Hydroxamic Acids and Carboxylic Acids

1990 ◽  
Vol 45 (8) ◽  
pp. 1123-1127 ◽  
Author(s):  
M. K. Das ◽  
S. Chakraborty
Keyword(s):  
Carboxylic Acid ◽  
Boric Acid ◽  
General Formula ◽  
Carboxylic Acids ◽  
Hydroxamic Acid ◽  
Hydroxamic Acids ◽  
Uv Spectra ◽  
Elemental Analyses

A number of boron spirochelates of the general formula B[R′CON(R)O]Y have been synthesized by the single-pot reaction of boric acid, a hydroxamic acid R′CON(R)OH and a carboxylic acid H2Y. The spirochelates have been characterized by elemental analyses, by IR, NMR (1H and 11B) and UV spectra and conductance measurements. They are non-electrolytes.

scholarly journals Microcrater-Arrayed Chemiluminescence Cell Chip to Boost Anti-Cancer Drug Administration in Zebrafish Tumor Xenograft Model

Biology ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 4
Author(s):  
Ching-Te Kuo ◽  
Yu-Sheng Lai ◽  
Siang-Rong Lu ◽  
Hsinyu Lee ◽  
Hsiu-Hao Chang
Keyword(s):  
Drug Screening ◽  
Cell Biology ◽  
Xenograft Model ◽  
Tumor Xenograft ◽  
Cancer Drug ◽  
Direct Writing ◽  
Drug Synergy ◽  
Optimal Drug ◽  
Anti Cancer ◽  
Mcf 7

Purpose: The aim of this study was to develop a rapid and automatic drug screening platform using microcrater-arrayed (µCA) cell chips. Methods: The µCA chip was fabricated using a laser direct writing technique. The fabrication time required for one 9 × 9 microarray wax chip was as quick as 1 min. On a nanodroplet handling platform, the chip was pre-coated with anti-cancer drugs, including cyclophosphamide, cisplatin, doxorubicin, oncovin, etoposide, and 5-fluorouracil, and their associated mixtures. Cell droplets containing 100 SK-N-DZ or MCF-7 cells were then loaded onto the chip. Cell viability was examined directly through a chemiluminescence assay on the chip using the CellTiter-Glo assay. Results: The time needed for the drug screening assay was demonstrated to be less than 30 s for a total of 81 tests. The prediction of optimal drug synergy from the µCA chip was found by matching it to that of the zebrafish MCF-7 tumor xenograft model, instead of the conventional 96-well plate assay. In addition, the critical reagent volume and cell number for each µCA chip test were 200 nL and 100 cells, respectively, which were significantly lower than 100 µL and 4000 cells, which were achieved using the 96-well assay. Conclusion: Our study for the µCA chip platform could improve the high-throughput drug synergy screening targeting the applications of tumor cell biology.

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