Design and Synthesis of New Phthalazinone Derivatives Containing Benzyl Moiety with Anticipated Antitumor Activity

Marzouk, Magda I.; Shaker, Soheir A.; Hafiz, Aisha Ali Abdel; El-Baghdady, Khaled Z.

doi:10.1248/bpb.b15-00656

Cited by 26 publications

(16 citation statements)

References 46 publications

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“…The synthesized compounds were tested for antimicrobial, cytotoxic, and antioxidant activities. Some of the compounds were showed very strong cytotoxic activity with respect to the standard (Marzouk et al, 2016). The study aims to synthesize phthalazine derivatives and to test their antiinflammatory and anti-proliferative activities.…”

Section: Pharmacological Activitiesmentioning

confidence: 99%

Pharmacological activities of various phthalazine and phthalazinone derivatives

Int¹

2019

Preprint

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Various pthalazine derivatives have been synthesized and tested for their diverse biological activities. Pthalazine derivatives have been exhibited pharmacological activities like antitumor, PARP-1 inhibitors, antimicrobial, antivirus, antihistamine-H1, antiallergic rhinitis, antifungal, anti-inflammatory, anti-proliferative, COX-2 inhibitor, LOX-5 inhibitor, antidiabetes, and other biological activities like imaging agent. Pthalazine derivatives were also used as agrochemicals and chemicals. Various synthetic aspects indicate that pthalazines derivatives are easy to synthesize which can produce a wide variety of activity.

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Section: Pharmacological Activitiesmentioning

confidence: 99%

Pharmacological activities of various phthalazine and phthalazinone derivatives

Int¹

2019

Preprint

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“…In the light of these facts, and as a continuation of our efforts towards synthesizing biologically active heterocyclic compounds especially those with antitumor activity [58][59][60][61][62], we planned to synthesize new hydrazide and 1,3,4-oxadiazole derivatives in the hope that new antitumor agents might be discovered. Hydrazides are very useful starting materials for the construction of several heterocyclic compounds such as 1,3,4-oxadiazoles [13], 1,3-thiazoles [14], 1,3,4-thiadiazoles [15], 1,2,4-triazoles [16] [18], pyrroles [19] and pyrazoles [20].…”

Section: (Figure 2) Also N-(5-(cyano(4-methyl-3-phenylthiazol-2(3h)-mentioning

confidence: 99%

Section: (Figure 2) Also N-(5-(cyano(4-methyl-3-phenylthiazol-2(3h)-mentioning

confidence: 99%

Utilization of Cyanoacetohydrazide and Oxadiazolyl Acetonitrile in the Synthesis of Some New Cytotoxic Heterocyclic Compounds

Shaker

Marzouk

2016

Molecules

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A (pyridazinyl)acetate derivative was reacted with thiosemicarbazide and hydrazine hydrate to yield spiropyridazinone and acetohydrazide derivatives, respectively. The acetohydrazide derivative was used as a starting material for synthesizing some new heterocyclic compounds such as oxoindolinylidene, dimethylpyrazolyl, methylpyrazolyl, oxopyrazolyl, cyanoacetylacetohydrazide and oxadiazolylacetonitrile derivatives. The behavior of the cyanoacetylacetohydrazide and oxadiazolylacetonitrile derivatives towards nitrogen and carbon nucleophiles was investigated. The assigned structures of the prepared compounds were elucidated by spectral methods (IR, 1 H-NMR 13 C-NMR and mass spectroscopy). Some of the newly prepared compounds were tested in vitro against a panel of four human tumor cell lines, namely hepatocellular carcinoma (liver) HePG-2, colon cancer HCT-116, human prostate cancer PC3, and mammary gland breast MCF-7. Also they were tested as antioxidants. Almost all of the tested compounds showed satisfactory activity.

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“…Phthalazinones exhibit ad iverse range of pharmaceutical properties, such as anti-cancer, [1][2][3] anti-inflammatory, [4][5][6] anti-bacterial, [1,7] anti-oxidant, [1] and anti-neurodegenerative [8] properties, with mechanismso fa ction that are as varied as the diseases they are used against. [9][10][11][12] For example, the clinically used anticancer drug oliparib (1,F igure 1) inhibits the poly(ADP-ribose)polymerase, [9] while azelastine (2)i sa na ntihistamine preferentially taken up by lung and alveolar macrophages.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Investigation of Phthalazinones as Antitubercular Agents

Santoso

Cheung

Hards

et al. 2019

Chemistry An Asian Journal

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A series of 2‐ and 7‐substituted phthalazinones was synthesised and their potential as anti‐tubercular drugs assessed via Mycobacterium tuberculosis (mc26230) growth inhibition assays. All phthalazinones tested showed growth inhibitory activity (MIC <100 μm), and those compounds containing lipophilic and electron‐withdrawing groups generally exhibited better anti‐tubercular activity. Several lead compounds were identified, including 7‐((2‐amino‐6‐(4‐fluorophenyl)pyrimidin‐4‐yl)amino)‐2‐heptylphthalazin‐1(2H)‐one (MIC=1.6 μm), 4‐tertbutylphthalazin‐2(1H)‐one (MIC=3 μm), and 7‐nitro‐phthalazin‐1(2H)‐one (MIC=3 μm). Mode of action studies indicated that selected pyrimidinyl‐phthalazinones may interfere with NADH oxidation, however, the mode of action of the lead compound is independent of this enzyme. MIC=minimum inhibitory concentration.

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Design and Synthesis of New Phthalazinone Derivatives Containing Benzyl Moiety with Anticipated Antitumor Activity

Cited by 26 publications

References 46 publications

Pharmacological activities of various phthalazine and phthalazinone derivatives

Pharmacological activities of various phthalazine and phthalazinone derivatives

Utilization of Cyanoacetohydrazide and Oxadiazolyl Acetonitrile in the Synthesis of Some New Cytotoxic Heterocyclic Compounds

Synthesis and Investigation of Phthalazinones as Antitubercular Agents

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