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

doi:10.3390/molecules16075840

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

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

Nageswara Rao Kode and Shashikant Phadtare*

Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA

* Author to whom correspondence should be addressed.

Received: 20 June 2011 / Accepted: 29 June 2011 / Published: 11 July 2011

(This article belongs to the Section Medicinal Chemistry)

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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

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Cite This Article

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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