SYNTHESIS AND ANTICANCER ACTIVITY EVALUATION OF SOME SCHIFF BASES OF 1, 3, 4-OXADIAZOLE

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 12-17
Author(s):  
Manpreet Kaur ◽  
S. Singh ◽  
Keyword(s):  
Schiff Base ◽  
Growth Inhibition ◽  
Anticancer Activity ◽  
Maximum Growth ◽  
Schiff Base Derivatives ◽  
Control Growth ◽  
Anti Cancer ◽  
Oxadiazole Derivatives ◽  
Cancer Activity ◽  
Mcf 7

A new series of 2,5-disubstituted-1,3,4-oxadiazole derivatives has been synthesized with the help of different aromatic benzaldehydes and final compounds were characterized by FTIR and 1H NMR. 2,5- disubstituted-1,3,4-oxadiazole derivatives were synthesized by the reaction of Schiff base derivatives with 2,5-disubstituted-1,3,4-oxadiazoles. All the synthesized compounds were screened for their anticancer activity. These compounds were evaluated for their anticancer activity against various cancer cell lines. Five of the compounds possessed good to moderate anti-cancer activity. Three of the synthesized compounds i.e. 6a, 6f and 6g were found to possess maximum growth inhibition. The order for the % control growth inhibition of MCF-7 was found to be 6a>6f>6g>5b>6h, as shown in Table II-VI.

SYNTHESIS, SPECTRAL CHARACTERIZATION AND ANTICANCER EVALUATION OF NEW DIAZENYL SCHIFF BASE DERIVATIVES

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 20-28
Author(s):  
P. K. N. Sarangi ◽  
◽  
J. Sahoo ◽  
S. K Paidesetty ◽  
G. P. Mohanta
Keyword(s):  
Schiff Base ◽  
Anticancer Activity ◽  
Cell Line ◽  
Leukemia Cell ◽  
Cancer Cell Line ◽  
Leukemia Cell Line ◽  
Primary Amines ◽  
Schiff Base Derivatives ◽  
Mcf 7

A series of several diazenyl Schiff base derivatives were designed and synthesized through azo coupling of diazotised primary amines with the novel synthesized Schiff base ligand (E)-N-((2-chloroquinolin-3-yl) methylene)-4-phenylthiazol-2-amine. All the synthesized compounds have been analysed by different spectral techniques such as elemental analysis, 1H NMR, FT-IR, UV-Vis and LC-MS for their structural confirmation. The above conjugates have been studied for their solvent effects by treating them with different solvents. The results of in vitro cytotoxic study of the synthesized compounds against MCF 7 (human breast cancer cell line) and K562 (Chronic Myeloid Leukemia cell line) revealed that some of the compounds show cytotoxic effect. However, the compounds (NZ)-N-(((4-bromo-3-methylphenyl) diazenyl) (2-chloroquinolin-3-yl) methylene)-4-phenylthiazol-2-amine: (5d) and 4-(((Z)-(2-chloroquinolin-3- yl)(4-phenylthiazol-2-ylimino)methyl)diazenyl)phenol (5e) showed potent cytotoxic activity in comparison to other compounds against MCF 7. Corroborating the results of anticancer activity, it is found to be observed that the compound 4- (((Z)- (2-chloroquinolin-3-yl) (4-phenylthiazol-2-ylimino)methyl) diazenyl) phenol (5e) showed excellent anticancer activity against MCF 7, which is further justified by the apoptosis study through Annexin V-FITC/PI analysis.

scholarly journals Synthesis of Novel Amide Functionalized Pyrido[2,3-d]pyrimidine Derivatives and their Anticancer Activity

2021 ◽  
Vol 33 (7) ◽  
pp. 1579-1584
Author(s):  
Chiranjeevi Abba ◽  
Naveen Puram ◽  
Sailu Betala
Keyword(s):  
Anticancer Activity ◽  
Human Cancer ◽  
Aromatic Aldehydes ◽  
Pyrimidine Derivatives ◽  
Human Cancer Cell Lines ◽  
Schiff Base Derivatives ◽  
Amide Derivatives ◽  
Anti Cancer ◽  
A549 Lung ◽  
Cancer Activity

A series of novel amide functionalized pyrido[2,3-d]pyrimidine derivatives were synthesized from 2-amino-6-(thiophen-2-yl)-4-(trifluoro-methyl)nicotinonitrile (1), which on reaction with trifluoroacetic acid to get pyridopyrimidine (2). Compound 2 when treated with bromoethyl acetate followed by hydrazine hydrate to get hydrazide derivatives 4. Compound 4 on reaction with different substituted aromatic aldehydes to obtain Schiff base derivatives 5a-f. In another way, compound 3 treated with different substituted amines and amino acids to obtain amide derivatives 6a-f, 7a-d and 8a-c. All the compounds evaluated for anti-cancer activity against four human cancer cell lines such as A549-Lung cancer (CCL-185), MCF7-Breast cancer (HTB-22), DU145-prostate cancer (HTB-81) and HeLa-cervical cancer (CCL-2) and among the sythesized compounds, only 5d, 7d and 8a were identified as the potent compounds against the anticancer activity.

Biological promiscuity of a binuclear Cu(ii) complex of aminoguanidine Schiff base: DNA binding, anticancer activity and histidine sensing ability of the complex

2020 ◽  
Vol 44 (18) ◽  
pp. 7319-7328
Author(s):  
Antu Mondal ◽  
Chandrima Das ◽  
Montse Corbella ◽  
Antonio Bauzá ◽  
Antonio Frontera ◽  
...  
Keyword(s):  
Schiff Base ◽  
Dna Binding ◽  
Anticancer Activity ◽  
Binding Activity ◽  
Fluorometric Determination ◽  
Dna Binding Activity ◽  
Anti Cancer ◽  
Cancer Activity

A binuclear Cu(ii) complex of aminoguanidine shows strong DNA binding activity and encouraging anti-cancer activity against HCT-16 cells. The complex can also be used for selective spectrophotomteric or fluorometric determination of histidine.

Schiff Bases and Complexes: A Review on Anti-Cancer Activity

2020 ◽  
Vol 20 (16) ◽  
pp. 1908-1917
Author(s):  
Garima Matela
Keyword(s):  
Inorganic Chemistry ◽  
Schiff Base ◽  
Side Effects ◽  
Antitumor Activity ◽  
Anticancer Activity ◽  
Schiff Bases ◽  
Tumor Cell Lines ◽  
Anti Cancer ◽  
New Anticancer Drugs ◽  
Cancer Activity

Development in the field of bio-inorganic chemistry increased the interest in Schiff base and its complexes due to its biological importance in many fields, including anticancer activity. Discovery of the antitumor activity of Schiff base and its complexes against various tumor cell lines fascinates the researchers to develop new anticancer drugs without any side effects. Thus, the present review focuses on the anticancer activity of Schiff bases and their metal complexes.

Synthesis and Anticancer Activity of 9-O-Pyrazole Alkyl Substituted Berberine Derivatives

2019 ◽  
Vol 18 (11) ◽  
pp. 1639-1648 ◽  
Author(s):  
Daipeng Xiao ◽  
Fen He ◽  
Dongming Peng ◽  
Min Zou ◽  
Junying Peng ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Molecular Docking ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Human Lung Cancer ◽  
Drug Candidate ◽  
Molecular Docking Study ◽  
Protective Function ◽  
Anti Cancer ◽  
Cancer Activity

Background: Berberine (BBR), an isoquinoline plant alkaloid isolated from plants such as Coptis chinensis and Hydrastis canadensis, own multiple pharmacological activities. Objective: In this study, seven BBR derivatives were synthesized and their anticancer activity against HeLa cervical and A549 human lung cancer cell lines were evaluated in vitro. Methods: The anti-cancer activity was measured by MTT assay, and apoptosis was demonstrated by the annexin V-FITC/PI staining assay. The intracellular oxidative stress was investigated through DCFH-DA assay. The molecular docking study was carried out in molecular operating environment (MOE). Results: Compound B3 and B5 showed enhanced anti-cancer activity compared with BBR, the IC50 for compound B3 and B5 were significantly lower than BBR, and compound B3 at the concentration of 64 or 128 µM induced apoptosis in HeLa and A549 cell lines. The reactive oxygen species (ROS) was generated in both cell lines when treated with 100 µM of all the compounds, and compound B3 and B5 induced higher activity in the generation of ROS, while compound B3 exhibited the highest activity, these results are in accordance with the cytotoxicity results, indicating the cytotoxicity were mostly generated from the oxidative stress. In addition, molecular docking analysis showed that compound B3 had the greatest affinity with Hsp90. Upon binding, the protective function of Hsp90 was lost, which might explain its higher cytotoxicity from molecular interaction aspect. Conclusion: All the results demonstrated that compound B3 and B5 showed significantly higher anti-cancer ability than BBR, and compound B3 is a promising anticancer drug candidate.

Poly(HPMA)–chlorambucil conjugate nanoparticles: facile fabrication and in vitro anti-cancer activity

2021 ◽  
Vol 45 (39) ◽  
pp. 18544-18551
Author(s):  
Guichen Li ◽  
Minzhi Zhao ◽  
Jia Zhang ◽  
Haining Li ◽  
Weibing Xu ◽  
...  
Keyword(s):  
Antitumor Effect ◽  
Anti Cancer ◽  
Facile Fabrication ◽  
Cancer Activity ◽  
Mcf 7

An acid-sensitive poly(HPMA)–Chl conjugate was developed and its antitumor effect towards HepG2 and MCF-7 cells was evaluated.

Curcumin Increases Anti-Cancer Activity of Tamoxifen in MCF-7 Breast Cancer Cells Through the Suppression of MDR1 mRNA Expression

2017 ◽  
Vol 23 (7) ◽  
pp. 6838-6840
Author(s):  
Melva Louisa ◽  
Lies Sugiarti ◽  
Sandy Vitria Kurniawan ◽  
Septelia Inawati Wanandi
Keyword(s):  
Breast Cancer ◽  
Mrna Expression ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Anti Cancer ◽  
Mdr1 Mrna ◽  
Cancer Activity ◽  
Mcf 7

scholarly journals Recent study on the anticancer activity of nobiletin and its metabolites

2021 ◽  
Vol 14 ◽  
Author(s):  
Ke Lv ◽  
Lingling Zhang ◽  
Hui Zhao ◽  
Chi-Tang Ho ◽  
Shiming Li
Keyword(s):  
Cancer Prevention ◽  
Anticancer Activity ◽  
Promising Candidate ◽  
Naturally Occurring ◽  
Antitumor Potential ◽  
Anti Cancer ◽  
Citrus Peels ◽  
Derivatives Of ◽  
Cancer Activity

The exploration of naturally occurring phytochemicals with antitumor potential has been the focus of many studies. Nobiletin, a polymethoxyflavone (PMF) exclusively derived from citrus peels, has been reported as a promising candidate for the prevention and/or treatment of cancers. Additionally, multiple demethylated derivatives of nobiletin from in vivo biotransformation, including 3′-demethylnobiletin (3′-DMN), 4′-demethylnobiletin (4′-DMN), 3′,4′-didemethylnobiletin (3′,4′-DDMN) and 5-demethylnobiletin (5-DMN), among others, have been found to show anti-cancer activity. In this review, the anticancer activity of nobiletin and its derivatives in cancer prevention are comprehensively described.

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