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

Patrick J Hrdlicka; Jan S Jepsen; Jesper Wengel; Jan Stenvang

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

Patrick J Hrdlicka, Jan S Jepsen, Jesper Wengel, Jan Stenvang

5 Citations (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.

Original language	English
Journal	Nucleosides, nucleotides & nucleic acids
Volume	24
Issue number	5-7
Pages (from-to)	397-400
Number of pages	4
ISSN	1525-7770
Publication status	Published - 2005

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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Synthesis and biological evaluation of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd). / Hrdlicka, Patrick J; Jepsen, Jan S; Wengel, Jesper et al.
In: Nucleosides, nucleotides & nucleic acids, Vol. 24, No. 5-7, 2005, p. 397-400.

Research output: Contribution to journal › Journal article › Research › 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",

author = "Hrdlicka, {Patrick J} and Jepsen, {Jan S} and Jesper Wengel and Jan Stenvang",

year = "2005",

language = "English",

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pages = "397--400",

journal = "Nucleosides, nucleotides & nucleic acids",

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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 - Jepsen, Jan S

AU - Wengel, Jesper

AU - Stenvang, Jan

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

SN - 1525-7770

VL - 24

SP - 397

EP - 400

JO - Nucleosides, nucleotides & nucleic acids

JF - Nucleosides, nucleotides & nucleic acids

IS - 5-7

ER -

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

Abstract

Keywords

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