Pharmacological and Clinical Studies on Purine Nucleoside Analogs- New Anticancer Agents

A series of 6-(4-substituted phenyl)-9-(tetrahydropyran-2-yl)purines 3-9, 6-(4-substituted phenyl)purines 10-16, 9-((4-substituted phenyl)sulfonyl)-6-(4-substituted phenyl)purines 17-32 were prepared and screened initially for their in vitro anticancer activity against selected human cancer cells (liver Huh7, colon HCT116, breast MCF7). 6-(4-Phenoxyphenyl)purine analogues 9, 16, 30-32, had potent cytotoxic activities. The most active purine derivatives 5-9, 14, 16, 18, 28-32 were further screened for their cytotoxic activity in hepatocellular cancer cells. 6-(4-Phenoxyphenyl)-9-(tetrahydropyran-2-yl)-9H-purine (9) had better cytotoxic activity (IC 50 5.4 μM) than the well-known nucleobase analogue 5-FU and known nucleoside drug fludarabine on Huh7 cells. The structure-activity relationship studies reported that the substitution at C-6 positions in purine nucleus with the 4-phenoxyphenyl group is responsible for the anti-cancer activity.

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“…3) were approved in FDA for the therapy of hematologic disorders between 1991 and 1992. 18,19 2. Experimental…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Some Substituted 6-Phenyl Purine Analogues and Their Biological Evaluation as Cytotoxic Agents

Küçükdumlu

Tunçbìlek²,

Güven³

et al. 2017

ACSi

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Section: Introductionmentioning

confidence: 99%

“…Cells obtain purine nucleotides through two separate metabolic pathways, de novo purine synthesis and salvage of extracellular purine bases and nucleotides [2]. Therefore, de novo purine synthesis and several enzymes involved in the purine metabolism pathway are important targets for antimetabolites [2]. Purine antimetabolites have been used in the development of many potent medicinal agents, which exhibited antineoplastic, antileukemic, antiviral, antibacterial, and antifungal activities [1][2][3][4].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 9-Substituted Derivatives of tert-Butyl 6-(9h-Purin-6-Ylthio) Hexylcarbamate

P¹

2013

Med chem

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“…1) Cells obtain purine nucleotides through two separate metabolic pathways, de novo purine synthesis and salvage of extracellular purine bases. 2) Therefore, de novo purine syntheses are important targets for antimetabolites. 3) Purine antimetabolites are of great importance to chemists as well as to biologists as they possess antitubercular, antiulcer, antimicrobial, antifungal, antineoplastic, antitumor, antiviral and cardiotonic properties.…”

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confidence: 99%

Synthesis of Some Novel Thiocyanotopurine Derivatives and Investigation of Their Antimicrobial Activity and DNA Interactions

Çelik

Dişli

Öner

et al. 2012

CHEMICAL & PHARMACEUTICAL BULLETIN

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A series of 6-thiocyanatopurine derivatives introduced with different alkyl groups in position 9 was synthesized. The structures of the synthesized compounds were evaluated via spectroscopic methods and elemental methods of analyses. All the synthesized compounds were screened for their antibacterial activities against Gram-positive and Gram-negative bacteria and for their antifungal activities against yeast strains. All the synthesized compounds showed better antibacterial activities against Gram-positive bacteria compared to Gram-negative bacteria. DNA interactions with pBR322 DNA were determined. Most of the compounds caused conformational changes in DNA.Key words purine derivative; antimetabolite; antimicrobial activity; DNA interaction Purines are one of the most important classes of heterocyclic compounds in nature, fulfilling functional roles as nucleic acids, coenzymes, and constituents in metabolic processes, cell signaling, and energy storage.

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Pharmacological and Clinical Studies on Purine Nucleoside Analogs- New Anticancer Agents

Cited by 35 publications

References 34 publications

Synthesis of Some Substituted 6-Phenyl Purine Analogues and Their Biological Evaluation as Cytotoxic Agents

Synthesis of Some Substituted 6-Phenyl Purine Analogues and Their Biological Evaluation as Cytotoxic Agents

Synthesis of 9-Substituted Derivatives of tert-Butyl 6-(9h-Purin-6-Ylthio) Hexylcarbamate

Synthesis of Some Novel Thiocyanotopurine Derivatives and Investigation of Their Antimicrobial Activity and DNA Interactions

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