The anticancer potential of various substituted  pyridazines and related compounds

Asif, Mohammad

doi:10.14419/ijac.v2i2.2661

Cited by 12 publications

(4 citation statements)

References 61 publications

(42 reference statements)

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“…Pyridazine-based frameworks are widely distributed in biologically active products with anti-viral [ 15 , 16 , 17 , 18 , 19 , 20 ], anti-inflammatory [ 21 , 22 , 23 , 24 , 25 ], anti-microbial [ 26 , 27 , 28 ], anti-cancer [ 29 , 30 , 31 , 32 , 33 , 34 , 35 , 36 ], anti-convulsant [ 37 , 38 , 39 , 40 ], anti-analgesic [ 41 , 42 ], anti-tubercular [ 43 , 44 , 45 ], anti-hypertensive [ 3 , 46 ], anti-diabetic [ 47 ], anti-depressant [ 48 , 49 ], anti-Alzheimer’s [ 50 , 51 ], phosphodiesterase [ 52 , 53 ], platelet aggregation [ 54 , 55 , 56 , 57 ], and cholesterol acyl transferase inhibitor properties [ 58 ]. Peptide nucleic acids (PNAs) with new pyridazine-type nucleobases were reported as replacements for the DNA duplex bases instead of thymine, adenine, guanine and cytosine to form novel DNA or RNA duplexes [ 59 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Some New Pyridazine Derivatives for Anti-HAV Evaluation

et al. 2017

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4-(2-(4-Halophenyl)hydrazinyl)-6-phenylpyridazin-3(2H)-ones 1a,b were prepared and treated with phosphorus oxychloride, phosphorus pentasulphide and ethyl chloroformate to give the corresponding chloropyridazine, pyridazinethione, oxazolopyridazine derivatives 2–4, respectively. Compound 2 reacted with hydrazine hydrate to afford hydrazinylpyridazine 7. The reaction of 4-(2-(4-chlorophenyl)hydrazinyl)-3-hydrazinyl-6-phenylpyridazine (7) with acetic anhydride, p-chlorobenzaldehyde and carbon disulphide gave the corresponding pyridazinotriazine derivatives 8–10. On the other hand, 5-(4-chlorophenylamino)-7-(3,5-dimethoxybenzylidene)-3-phenyl-5H-pyridazino[3,4-b][1,4]thiazin-6(7H)-one (11) was prepared directly from the reaction of compound 3 with chloroacetic acid in presence of p-chlorobenzaldehyde. Compound 11 reacted with nitrogen nucleophiles (hydroxylamine hydrochloride, hydrazine hydrate) and active methylene group-containing reagents (malononitrile, ethyl cyanoacetate) to afford the corresponding fused compounds 12–15, respectively. Pharmacological screening for antiviral activity against hepatitis A virus (HAV) was performed for the new compounds. 4-(4-Chlorophenylamino)-6-phenyl-1,2-dihydropyridazino[4,3-e][1,2,4]triazine-3(4H)-thione (10) showed the highest effect against HAV.

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Section: Introductionmentioning

confidence: 99%

Synthesis of Some New Pyridazine Derivatives for Anti-HAV Evaluation

et al. 2017

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“…Pyridazinone derivatives have gained substantial attention within the field of medicinal chemistry. Pyridazine moiety has been tested extensively for its diverse biological activities including antiinflammatory, analgesic, anticancer, antiviral, antimicrobial, cardiovascular, antitubercular, antiobesity, antidiabetic, neuroprotective, and various other activities [90][91][92][93][94][95][96]. Cardiovascular diseases (CVDs) are the leading reason for death worldwide and remain the leading reason for avoidable death worldwide.…”

Section: Discussionmentioning

confidence: 99%

A Review on Pyridazinone Ring Containing Various Cardioactive Agents

Asif

2019

J. Chem. Rev.

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In this work, some pyridazinones were studied for their cardioactive activity. These compounds showed significant cardio-active action with respect to the regular used drugs. However, it was found that the existence of the pyridazine ring is a crucial necessity in the structure of these pyridazinonecompounds to show the improved cardioactive activities. It was also understood that the substitution of the different group on the pyridazinone ring with other related bioisosteres or isosteres along with the existence of pyridazine ring may provide better cardioactive compounds. Pyridazinoneis, a component of various cardio-active agents, which are in uses clinically or in clinical trials. These contain pimobendan, indolidan, levosimendan, imazodan, CI-930, meribendan, bemoradan, senazodan, siguazodan, amipizone, prinoxodan, Y-590, SK&F-93741, SKF 95654, NSP-805, NSP-804 and KF 15232. This study briefly reviews the pyridazinone ring for the progress of new cardio-active drugs.

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“…Recently, it was reported that some pyridazin-3(2h)-one derivatives specifically interact with and inhibit PIM (potential tumor targets) kinases with low nanomolar potency [18][19][20][21]. In addition, pyridazin-3(2h)-ones are endowed by many biological activities [22][23][24]. In this context, the present study was aimed at synthesizing new pyridazin-3(2h)-one derivatives with cytotoxic activity.…”

Section: Introductionmentioning

confidence: 99%

Reactive Oxygen Species-Mediated Apoptosis and Cytotoxicity of Newly Synthesized Pyridazin-3-Ones In P815 (Murin Mastocytoma) Cell Line

et al. 2019

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Background In cancer cells, the intracellular antioxidant capacity and the redox homeostasis are mainly maintained by the glutathione- and thioredoxin-dependent systems which are considered as promising targets for anticancer drugs. Pyridazinones constitute an interesting source of heterocyclic compounds for drug discovery. The present investigation focused on studying the in-vitro antitumor activity of newly synthesized Pyridazin-3(2h)-ones derivatives against P815 (Murin mastocytoma) cell line. Methods The in-vitro cytotoxic activities were investigated toward the P815 cell line using tetrazolium-based MTT assay. Lipid peroxidation and the specific activities of antioxidant enzymes were also determined. Results The newly compounds had a selective dose-dependent cytotoxic effect without affecting normal cells (PBMCs). Apoptosis was further confirmed through the characteristic apoptotic morphological changes and DNA fragmentation. Two compounds (6f and 7h) were highly cytotoxic and were submitted to extend biological testing to determine the likely mechanisms of their cytotoxicity. Results showed that these molecules may induce cytotoxicity via disturbing the redox homeostasis. Importantly, the anticancer activity of 6f and 7h could be due to the intracellular reactive oxygen species hypergeneration through significant loss of glutathione reductase and thioredoxin reductase activities. This eventually leads to oxidative stress-mediated P815 cell apoptosis. Furthermore, the co-administration of 6f or 7h with Methotrexate exhibited a synergistic cytotoxic effect. Conclusions considering their significant anticancer activity and chemosensitivity, 6f and 7h may improve the therapeutic efficacy of the current treatment for cancer.

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The anticancer potential of various substituted pyridazines and related compounds

Cited by 12 publications

References 61 publications

Synthesis of Some New Pyridazine Derivatives for Anti-HAV Evaluation

Synthesis of Some New Pyridazine Derivatives for Anti-HAV Evaluation

A Review on Pyridazinone Ring Containing Various Cardioactive Agents

Reactive Oxygen Species-Mediated Apoptosis and Cytotoxicity of Newly Synthesized Pyridazin-3-Ones In P815 (Murin Mastocytoma) Cell Line

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