Synthesis of novel 6-substituted amino-9-(beta-D-ribofuranosyl)purine analogs and their bioactivities on human epithelial cancer cells

Kucukdumlu, Asligul
Guven, Ebru Bilget
Altiparmak, Duygu
Atalay, Rengül
New nucleoside derivatives with nitrogen substitution at the C-6 position were prepared and screened initially for their in vitro anticancer bioactivity against human epithelial cancer cells (liver Huh7, colon HCT116, breast MCF7) by the NCI-sulforhodamine B assay. N-6-(4-trifluoromethylphenyl) piperazine analog (27) exhibited promising cytotoxic activity. The compound 27 was more cytotoxic (IC50 = 1-4 mu M) than 5-FU, fludarabine on Huh7, HCT116 and MCF7 cell lines. The most potent nucleosides (11, 13, 16, 18, 19, 21, 27, 28) were further screened for their cytotoxicity in hepatocellular cancer cell lines. The compound 27 demonstrated the highest cytotoxic activity against Huh7, Mahlavu and FOCUS cells (IC50 = 1, 3 and 1 mu M respectively). Physicochemical properties, drug-likeness, and drug score profiles of the molecules showed that they are estimated to be orally bioavailable. The results pointed that the novel derivatives would be potential drug candidates.


Synthesis of Some Substituted 6-Phenyl Purine Analogues and Their Biological Evaluation as Cytotoxic Agents
Kucukdumlu, Asligul; Tuncbilek, Meral; Guven, Ebru Bilget; Atalay, Rengül (2017-01-01)
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 t...
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Isolation and characterization of circulating tumor cells (CTCs) have important clinical significance in terms of prognosis and early detection of response to treatment. Moreover, downstream characterization of CTCs may help better patient stratification and therapy guidance. However, CTCs are extremely rare (~10 CTCs/1010 peripheral blood cells) and highly sensitive, and specific technology is required for their isolation. Rapidly developing microfluidic technologies offer variety of advantages in rare cel...
Citation Formats
M. TUNÇBİLEK, A. Kucukdumlu, E. B. Guven, D. Altiparmak, and R. Atalay, “Synthesis of novel 6-substituted amino-9-(beta-D-ribofuranosyl)purine analogs and their bioactivities on human epithelial cancer cells,” BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, pp. 235–239, 2018, Accessed: 00, 2020. [Online]. Available: