Synthesis and Anticancer Activity of New Hydrazide-hydrazones and Their Pd(II) Complexes

2019 ◽  
Vol 16 (5) ◽  
pp. 522-532 ◽  
Author(s):  
Bedia Kocyigit-Kaymakcioglu ◽  
Senem Sinem Yazici ◽  
Fatih Tok ◽  
Miriş Dikmen ◽  
Selin Engür ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cytotoxic Effect ◽  
A549 Cells ◽  
Cancer Cell Line ◽  
Fibroblast Cell ◽  
Reference Drug ◽  
A549 Cancer Cell Line

Background: Hydrazones, one of the important classes of organic molecules, are pharmaceutical agents comprising –CO-NH-N=CH- group in the structure therefore and exhibiting significant biological activity. Methods: 5-Chloro-N’-[(substituted)methylidene] pyrazine-2-carbohydrazide (3a-g) and their Pd(II) complexes (4a-h) were synthesized and investigated in vitro anticancer activity on A549, Caco2 cancer and normal 3T3 fibroblast cell lines, using the MTT assay. Results: Anticancer activity screening results revealed that some compounds showed remarkable cytotoxic effect. Among them, 5-chloro-N'-[(4-hydroxyphenyl)methylidene] pyrazine-2-carbohydrazide (3c) displayed higher cytotoxic activity against A549 cancer cell line than the reference drug cisplatin. Conclusion: Compound 3c showed high cytotoxic activity against A549 cancer cell line but it showed low cytotoxic effect against normal 3T3 fibroblast cell line. Antiproliferative and antimetastatic effects of 3c were determined by the real-time monitoring of cell proliferative system (RTCA DP). The cell proliferation, metastatic and invasive activities of A549 cells were decreased due to increased concentration of 3c.

Design, synthesis and biological evaluation of cyanopyridines, pyridopyrazolopyrimidines and pyridopyrazolotriazines as potential anticancer agents

2020 ◽  
Vol 17 ◽  
Author(s):  
Reda Mohammed Keshk ◽  
Batoul Mohamed Izzularab
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Normal Fibroblast ◽  
Cancer Resistance ◽  
Design Synthesis ◽  
Reference Drug ◽  
Chemical Structures

Background: The continuous need for new anticancer drugs is a never-ending task due to cancer resistance to the existing drugs. Objective: This article aimed to Design, synthesis, characterization, and anticancer evaluation of cyanopyridines, pyridopyrazolopyrimidines and pyridopyrazolotriazines. Materials and Methods: FTIR spectra were recorded on Thermo nioclet iso10 FT-IR. 1H and 13C NMR spectra were recorded on on JEOL (500 MHz) and Bruker 400 MHz spectrometer. Anticancer activity was determined using MTT assay against three cancer cell lines namely liver cancer cell line (HepG-2), pancreatic cancer cell line (PANC-1), non-small lung cancer cell line (A-549) and normal fibroblast. Results and Discussion: New series of 3-cyanopyridines (2a,b, 4, 5, 9), pyridopyrimidine (10), pyridopyrazolopyrimidines (11a-c, 12a,b, 18), pyrazolopyridine salt (13) and pyridopyrazolotriazines (16a,b) were synthesized from 3-cyano-4,6- dimethyl-2-pyridone. The novel synthesized compounds were evaluated in vitro for their anticancer activity and their chemical structures were determined by elemental analysis and spectroscopic data. Conclusion: The obtained data revealed that some of the synthesized compounds showed remarkable anticancer activities, especially 11a exhibited superior potency to the reference drug cisplatin against A-549 (IC50 = 9.24 µg mL-1 compared by 11.76 µg mL-1 for reference drug) and safe (IC50 = 66 µg mL-1) for normal fibroblast. Furthermore, compound 16a displayed the highest activity among the tested compounds against HepG-2 (IC50 = 6.45 µg mL-1 equipotent to cisplatin) with the highest safety profile (IC50=113.97 µg mL-1).

Cytotoxic and Apoptotic Effects of Novel Pyrrolo[2,3-d]Pyrimidine Derivatives Containing Urea Moieties on Cancer Cell Lines

2019 ◽  
Vol 18 (9) ◽  
pp. 1303-1312 ◽  
Author(s):  
Zühal Kilic-Kurt ◽  
Filiz Bakar-Ates ◽  
Bahriye Karakas ◽  
Özgür Kütük
Keyword(s):  
Cell Cycle ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
A549 Cells ◽  
Cancer Cell Line ◽  
Anticancer Activities ◽  
Cycle Arrest ◽  
Apoptotic Protein ◽  
Mcf 7

Background: Pyrrolo[2,3-d]pyrimidines have been recently reported to have anticancer activities through inhibition of different targets such as, Epidermal Growth Factor Receptor (EGFR) tyrosine kinase, Janus Kinase (JAK), mitotic checkpoint protein kinase (Mps1), carbonic anhydrase, MDM-2. On the other hand, aryl urea moieties which are found in some tyrosine kinase inhibitors such as Sorafenib and Linifanib have aroused recent attention as responsible for anticancer activities. The aims of this paper are to synthesize pyrrolo[ 2,3-d]pyrimidine derivatives containing urea moiety and evaluate their anti-cancer activity against human lung cancer cell line (A549), prostate cancer cell line (PC3), human colon cancer cell line (SW480) and human breast cancer cell line (MCF-7). Methods: A series of new pyrrolo[2,3-d]pyrimidines containing urea moieties have been synthesized as Scheme 1. In vitro cytotoxicity of target compounds were evaluated against, SW480, PC3, A549 and MCF-7 human cancer cell lines using a MTT assay. In order to evaluate the mechanism of cytotoxic activity of compounds 9e, 10a and 10b, having the best cytotoxic activity, Annexin V binding assay, cell cycle analysis and western blot analysis were performed. Results: Among the target compounds, 10a (IC50 = 0.19 µM) was found to be the most potent derivative against PC3 cells. Compound 10b and 9e showed the strong cytotoxic activity against MCF-7 and A549 cells with IC50 value of 1.66 µM and 4.55 µM, respectively. Flow cytometry data suggest that the cytotoxic activity of the compounds on cancer cells might be mediated by apoptosis revealing a significant increase in the percentage of late apoptotic cells and causing a cell cycle arrest at different stages. Western blot analysis of apoptosis marker demonstrated that these compounds induce apoptosis through the intrinsic pathway. Conclusion: Compound 9e displayed the strongest cytotoxicity against A549 cancer cell line, and induced late apoptosis in A549, as confirmed by cell cycle arrest in G0/G1 phase. In addition, compound 9e reduced expression of the anti-apoptotic protein Bcl-2 and enhanced expression of the pro-apoptotic protein Bax, besides increased caspase-9 and caspase-3, as well as cleavage of PARP levels. These results suggest that compound 9e showed a cytotoxic effect in A549 cells through activation of the mitochondrial apoptotic pathway. Further studies will be undertaken in our laboratory to improve cytotoxic activity of compound 9e and to identify the biological targets of 9e which are responsible for anticancer activity.

scholarly journals Cytotoxic Activity of Ethanolic Extract of Aloe saudiarabica and Aloe shadensis against Three Human Cancer Cell Line

2021 ◽  
pp. 138-146
Author(s):  
Awad A Algarni
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
A549 Cells ◽  
Cancer Cell Line ◽  
Human Cancer Cell ◽  
Main Compound ◽  
Mcf 7

Aloe saudiarabica and Aloe shadensis are a rare species of the genus Aloe found only in Saudi Arabia. The cytotoxic activity of both plants were evaluated in the current study using three different human cancer cell line, lung carcinoma (A-549), breast adenocarcinoma (MCF-7) and liver cancer (HepG2), assessed by WST-1 cell viability assays. The results indicate that the Aloe saudiarabica and Aloe shadensis showed weak cytotoxic effects against all three tested cancer cell lines, with an IC50 value of >300 μg/ml. In addition, HepG2 cells were more sensitive to Aloe saudiarabica treatment than MCF-7 and A549 cells, while MCF-7 cells were more sensitive to Aloe shadensis treatment than HepG2 and A549 cells. This study also identified the characteristic chemical constituents of the two plants using gas chromatography-mass spectrometry technique and the result indicated that 9-octadecenoic acid (Z)-, methyl ester (32.23%) was the main compound of Aloe saudiarabica while methyl 9-octadecenoate (17.28%) was the main compound of Aloe shadensis. In conclusion, the in vitro evaluation of Aloe saudiarabica and Aloe shadensis methanolic extraction showed low cytotoxicity on the viability of A-549, MCF-7 and HepG2 cell lines.

scholarly journals Correction: Gobinath, P., et al. Grindstone Chemistry: Design, One-Pot Synthesis, and Promising Anticancer Activity of Spiro[acridine-9,2′-indoline]-1,3,8-trione Derivatives against the MCF-7 Cancer Cell Line. Molecules 2020, 25, 5862

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1131
Author(s):  
Perumal Gobinath ◽  
Ponnusamy Packialakshmi ◽  
Ali Daoud ◽  
Saud Alarifi ◽  
Akbar Idhayadhulla ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
One Pot ◽  
One Pot Synthesis ◽  
Mcf 7

In the original article [...]

scholarly journals Promising Anticancer Activity of [Bis(1,8-quinolato)palladium (II)] Alone and in Combination

2020 ◽  
Author(s):  
Md. Nur Alam ◽  
Mohammad Moni ◽  
Jun Yu ◽  
Philip Beale ◽  
Peter Turner ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antitumour Activity ◽  
Epigallocatechin Gallate ◽  
Cancer Cell Line ◽  
Resistant Cell ◽  
Colorectal Cancer Cell Line

Abstract Due to similar coordination chemistry of palladium and platinum, a large number of palladium compounds too have been investigated for their anticancer activity. In the present study we describe synthesis, characterization and anticancer activity of palladium complex [Bis(1,8-quinolato)palladium (II)], coded as NH3 against seven different cancer cell lines. NH3 is found to have higher antitumour activity than cisplatin against both parent ovarian A2780 cell line and cisplatin-resistant cell lines. Also, NH3 has the lowest IC50 value against HT-29 colorectal cancer cell line. The higher antitumour activity of NH3 is due to the presence of bulky 8-hydroxy-quinoline ligand thus reducing its reactivity. Proteomic study has identified significantly expressed proteins which have been validated through bioinformatics. NH3 has been found to be less toxic than cisplatin at 2.5 mg/kg and 5 mg/kg dosages on mice models. Binary combinations of NH3 with curcumin and epigallocatechin gallate (EGCG) have demonstrated dose and sequence dependent synergism in ovarian and colorectal cancer models. All of the preclinical studies indicate promising therapeutic potentiality of NH3 [Bis(1,8-quinolato)palladium (II) ] as an anticancer drug.

Synthesis and cytotoxic activity of certain benzothiazole derivatives against human MCF-7 cancer cell line

2016 ◽  
Vol 89 (4) ◽  
pp. 566-576 ◽  
Author(s):  
Lamia W. Mohamed ◽  
Azza T. Taher ◽  
Ghada S. Rady ◽  
Mamdouh M. Ali ◽  
Abeer E. Mahmoud
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Benzothiazole Derivatives ◽  
Mcf 7
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