Purines and triazolo[4,3-e]purines containing pyrazole moiety as potential anticancer and antioxidant agents

Targeting apoptosis regulators such as caspases aiming at inducing apoptosis is an attractive strategy in cancer therapy. 8-Substituted purine incorporating pyrazole moiety were designed, synthesized and evaluated for their anticancer and antioxidant activities. Compounds and displayed potent and se...

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Bibliographic Details
Published in:Future medicinal chemistry 2018-06, Vol.10 (12), p.1449-1464
Main Authors: Shaaban, Omaima G, Abd El Razik, Heba A, A Shams El-Dine, Shams El-Dine, Ashour, Fawzia A, El-Tombary, Alaa A, Afifi, Ola S, Abu-Serie, Marwa M
Format: Article
Language:English
Subjects:
A549 Cells
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
antioxidant
Antioxidants - chemical synthesis
Antioxidants - chemistry
Antioxidants - pharmacology
apoptosis
Apoptosis - drug effects
caspase
Caspases - metabolism
Cell Line, Tumor
DNA Damage - drug effects
Drug Screening Assays, Antitumor
Humans
Neoplasms - drug therapy
Neoplasms - genetics
Neoplasms - metabolism
Neoplasms - pathology
purine
Purines - chemical synthesis
Purines - chemistry
Purines - pharmacology
pyrazole
Structure-Activity Relationship
Triazoles - chemical synthesis
Triazoles - chemistry
Triazoles - pharmacology
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Summary:Targeting apoptosis regulators such as caspases aiming at inducing apoptosis is an attractive strategy in cancer therapy. 8-Substituted purine incorporating pyrazole moiety were designed, synthesized and evaluated for their anticancer and antioxidant activities. Compounds and displayed potent and selective anticancer activity against lung cancer A549 cell line with low cytotoxicity on peripheral blood mononuclear normal cells. Compounds and induced caspase dependent apoptotic death and DNA damage in all cancer cell lines. In addition, compounds , , , , , , and showed good antioxidant activity higher than that of the standard ascorbic acid. Compounds and can be considered promising dual anticancer and antioxidant leads inducing caspase-dependent apoptotic death and DNA damage.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2017-0227