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Molecules 2011, 16(7), 5840-5860; doi:10.3390/molecules16075840
Article

Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines

 and *
Received: 20 June 2011; Accepted: 29 June 2011 / Published: 11 July 2011
(This article belongs to the Section Medicinal Chemistry)
Download PDF [433 KB, updated 18 June 2014; original version uploaded 18 June 2014]
Abstract: A seriesof twenty four acyclic unsaturated 2,6-substututed purines 5a-20b were synthesized. These compounds were evaluated for cytotoxic activity against NCI-60 DTP human tumor cell line screen at 10µMconcentration. N9-[(Z)-4'-chloro-2'-butenyl-1'-yl]-2,6-dichloropurine(5a), N9-[4'-chloro-2'-butynyl-1'-yl]-2,6-dichloropurine(10a), N9-[(E)-2',3'-dibromo-4'-chloro-2'-butenyl-1'-yl]-6-methoxypurine(14)and N9-[4'-chloro-2'-butynyl-1'-yl]-6-(4-methoxyphenyl)-purine(19)exhibited highly potent cytotoxic activity with GI50 values in the 1–5 µM range for most human tumor cell lines. Other compounds exhibited moderate activity.
Keywords: Suzuki-Miyaura cross coupling reaction; pyridiniumtribromide bromination; 2,6-substituted purines; cytotoxic activity Suzuki-Miyaura cross coupling reaction; pyridiniumtribromide bromination; 2,6-substituted purines; cytotoxic activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Kode, N.R.; Phadtare, S. Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines. Molecules 2011, 16, 5840-5860.

AMA Style

Kode NR, Phadtare S. Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines. Molecules. 2011; 16(7):5840-5860.

Chicago/Turabian Style

Kode, Nageswara Rao; Phadtare, Shashikant. 2011. "Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines." Molecules 16, no. 7: 5840-5860.


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