Synthesis and biological evaluation of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd)

Patrick J Hrdlicka; Jan Stenvang; Jesper Wengel

Synthesis and biological evaluation of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd)

Patrick J Hrdlicka, Jan Stenvang, Jesper Wengel

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

5 Citationer (Scopus)

Abstract

A series of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd) and its uracil analog (EUrd) have been synthesized. While none of the conformationally restricted analogs displayed anticancer activity, 5-iodo-EUrd and 5-bromo-EUrd displayed potent anticancer activity with IC50 values of 35 nM and 0. 73 microM.

Originalsprog	Engelsk
Tidsskrift	Nucleosides, nucleotides & nucleic acids
Vol/bind	24
Udgave nummer	5-7
Sider (fra-til)	397-400
Antal sider	4
ISSN	1525-7770
Status	Udgivet - 2005
Udgivet eksternt	Ja

Citationsformater

Synthesis and biological evaluation of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd). / Hrdlicka, Patrick J; Stenvang, Jan; Wengel, Jesper.

I: Nucleosides, nucleotides & nucleic acids, Bind 24, Nr. 5-7, 2005, s. 397-400.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

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abstract = "A series of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd) and its uracil analog (EUrd) have been synthesized. While none of the conformationally restricted analogs displayed anticancer activity, 5-iodo-EUrd and 5-bromo-EUrd displayed potent anticancer activity with IC50 values of 35 nM and 0. 73 microM.",

keywords = "Antimetabolites, Antineoplastic Agents, Cell Line, Tumor, Chemistry, Pharmaceutical, Cytidine, Drug Design, Drug Screening Assays, Antitumor, Humans, Inhibitory Concentration 50, Models, Chemical, Neoplasms, Nucleic Acid Conformation, Uracil, Uridine",

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T1 - Synthesis and biological evaluation of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd)

AU - Hrdlicka, Patrick J

AU - Stenvang, Jan

AU - Wengel, Jesper

PY - 2005

Y1 - 2005

N2 - A series of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd) and its uracil analog (EUrd) have been synthesized. While none of the conformationally restricted analogs displayed anticancer activity, 5-iodo-EUrd and 5-bromo-EUrd displayed potent anticancer activity with IC50 values of 35 nM and 0. 73 microM.

AB - A series of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd) and its uracil analog (EUrd) have been synthesized. While none of the conformationally restricted analogs displayed anticancer activity, 5-iodo-EUrd and 5-bromo-EUrd displayed potent anticancer activity with IC50 values of 35 nM and 0. 73 microM.

KW - Antimetabolites

KW - Antineoplastic Agents

KW - Cell Line, Tumor

KW - Chemistry, Pharmaceutical

KW - Cytidine

KW - Drug Design

KW - Drug Screening Assays, Antitumor

KW - Humans

KW - Inhibitory Concentration 50

KW - Models, Chemical

KW - Neoplasms

KW - Nucleic Acid Conformation

KW - Uracil

KW - Uridine

M3 - Journal article

C2 - 16247958

VL - 24

SP - 397

EP - 400

JO - Nucleosides, Nucleotides and Nucleic Acids

JF - Nucleosides, Nucleotides and Nucleic Acids

SN - 1525-7770

IS - 5-7

ER -