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

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.

2017 ◽  
Vol 12 (2) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Thao Quyen Cao ◽  
Bo Mi Lee ◽  
Yeon Woo Jung ◽  
Van Thu Nguyen ◽  
Jeong Ah Kim ◽  
...  

Cancer is a major public health burden in both developed and developing countries. Plant-derived compounds have played an important role in the development of useful anti-cancer agents. The current study was designed to evaluate the cytotoxic activity of chemical compounds from the stem bark of Styrax obassia. Seven known compounds (1–7) were isolated and identified. Compound 2 exhibited cytotoxic activity against the breast cancer cell line MCF-7 with an IC50 of 27.9 μM, followed by the human cervical cancer cell line Hela with an IC50 of 23.3 μM, and the human promyelocytic leukemia cell line HL-60 with an IC50 of 47.8 μM. Compound 7 exhibited cytotoxicity against Hela cells with an IC50 of 16.8 μM, followed by MCF-7 cells with an IC50 of 53.5 μM. This is the first study to investigate the significant anti-tumor properties of isolated compounds from the stem bark of S. obassia.


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.


2005 ◽  
Vol 28 (6) ◽  
pp. 646-647
Author(s):  
M Waheed Roomi ◽  
Vadim Ivanov ◽  
Aleksandra Niedzwiecki ◽  
Matthias Rath

2019 ◽  
Vol 26 (2) ◽  
pp. 1013-1020
Author(s):  
Robab Hassanvand Jamadi ◽  
Saeed Khalili ◽  
Tooba Mirzapour ◽  
Hashem Yaghoubi ◽  
Zahra Sadat Hashemi ◽  
...  

2021 ◽  
Vol Volume 15 ◽  
pp. 3523-3533
Author(s):  
Darwati Darwati ◽  
Ayu Nadila Safitri ◽  
Nurul Ambardhani ◽  
Tri Mayanti ◽  
Nurlelasari Nurlelasari ◽  
...  

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.


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