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Title of the item:

Design, Synthesis and In Vitro Cytotoxic Activity of New 6,9-Disubstituted Purine Analogues.

Title :
Design, Synthesis and In Vitro Cytotoxic Activity of New 6,9-Disubstituted Purine Analogues.
Authors :
Kucukdumlu A
Tuncbilek M
Guven EB
Atalay RC
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Source :
Acta chimica Slovenica [Acta Chim Slov] 2020 Mar; Vol. 67 (1), pp. 70-82.
Publication Type :
Journal Article
Language :
Imprint Name(s) :
Original Publication: Ljubljana : Slovenian Chemical Society,
MeSH Terms :
Antineoplastic Agents/*pharmacology
Antineoplastic Agents/chemical synthesis ; Cell Line, Tumor ; Cladribine/pharmacology ; Drug Design ; Drug Screening Assays, Antitumor ; Fluorouracil/pharmacology ; Humans ; Molecular Structure ; Purines/chemical synthesis ; Vidarabine/analogs & derivatives ; Vidarabine/pharmacology
Substance Nomenclature :
0 (Antineoplastic Agents)
0 (Purines)
47M74X9YT5 (Cladribine)
FA2DM6879K (Vidarabine)
P2K93U8740 (fludarabine)
U3P01618RT (Fluorouracil)
Entry Date(s) :
Date Created: 20210209 Date Completed: 20210813 Latest Revision: 20210813
Update Code :
Academic Journal
A series of new 6,9-disubstituted purine analogs with 4-substituted piperazine at C-6 and 4-substituted benzyl at N-9 were designed and synthesized in four steps. All synthesized compounds (7-26) were screened initially for their in vitro anticancer activity on Huh7 liver, HCT116 colon and MCF7 breast carcinoma cell lines. Cytotoxic bioactivity studies revealed that all compounds screened, with compound 19 being the exception, were found to have promising cytotoxic activities at IC50 range of 0.05-21.8 ∆M against cancer cells Huh7, HCT116 and MCF7. Among the prepared purine analogs, two of them (12 and 22) exhibited excellent cytotoxic activities, with IC50 0.08-0.13 ∆M, on Huh7 cells comparable to camptothecin (CPT) and better than cladribine, fludarabine and 5-FU. Afterwards, the evaluation of cytotoxicity of the most potent purine analogs was screened against further hepatocellular cancer (HCC) cell lines. The 6-(4-(4-trifluoromethylphenyl)piperazine (12) and 6-(4-(3,4-dichlorophenyl)piperazine analogs (25) displayed a significant IC50 values (IC50 < 0.1-0.13 ∆M) comparable to CPT and better cytotoxic bioactivity when compared with 5-FU, cladribine and fludarabine on HCC cells (Huh7 and HepG2).

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