Design, synthesis and evaluation of potent thymidylate synthase X inhibitors

F. Esra Önen; Yap Boum; Claire Jacquement; Maria Vittoria Spanedda; Nada Jaber; Daniel Scherman; Hannu Myllykallio; Jean Herscovici

doi:10.1016/j.bmcl.2008.04.080

Design, synthesis and evaluation of potent thymidylate synthase X inhibitors

F. Esra Önen
, Yap Boum
, Claire Jacquement
, Maria Vittoria Spanedda
, Nada Jaber
, Daniel Scherman
, Hannu Myllykallio
, Jean Herscovici

Research output: Contribution to journal › Article › peer-review

Abstract

Three synthesized series of compounds based on a thiazolidine core allowed identification of potent inhibitors of thymidylate synthase X. The evaluation of the catalytic activity of the enzyme in the presence of these molecules revealed two distinct classes of compounds that inhibit ThyX with submicromolar concentrations, which could lead, after optimization, to effective inhibitors with potential biomedical interest.

Original language	English
Pages (from-to)	3628-3631
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	12
DOIs	https://doi.org/10.1016/j.bmcl.2008.04.080
Publication status	Published - 15 Jun 2008
Externally published	Yes

Keywords

Antibacterial
Click chemistry
Thiazolidine
Thymidilate synthase
Triazole

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10.1016/j.bmcl.2008.04.080

Cite this

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abstract = "Three synthesized series of compounds based on a thiazolidine core allowed identification of potent inhibitors of thymidylate synthase X. The evaluation of the catalytic activity of the enzyme in the presence of these molecules revealed two distinct classes of compounds that inhibit ThyX with submicromolar concentrations, which could lead, after optimization, to effective inhibitors with potential biomedical interest.",

keywords = "Antibacterial, Click chemistry, Thiazolidine, Thymidilate synthase, Triazole",

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T1 - Design, synthesis and evaluation of potent thymidylate synthase X inhibitors

AU - Esra Önen, F.

AU - Boum, Yap

AU - Jacquement, Claire

AU - Spanedda, Maria Vittoria

AU - Jaber, Nada

AU - Scherman, Daniel

AU - Myllykallio, Hannu

AU - Herscovici, Jean

PY - 2008/6/15

Y1 - 2008/6/15

N2 - Three synthesized series of compounds based on a thiazolidine core allowed identification of potent inhibitors of thymidylate synthase X. The evaluation of the catalytic activity of the enzyme in the presence of these molecules revealed two distinct classes of compounds that inhibit ThyX with submicromolar concentrations, which could lead, after optimization, to effective inhibitors with potential biomedical interest.

AB - Three synthesized series of compounds based on a thiazolidine core allowed identification of potent inhibitors of thymidylate synthase X. The evaluation of the catalytic activity of the enzyme in the presence of these molecules revealed two distinct classes of compounds that inhibit ThyX with submicromolar concentrations, which could lead, after optimization, to effective inhibitors with potential biomedical interest.

KW - Antibacterial

KW - Click chemistry

KW - Thiazolidine

KW - Thymidilate synthase

KW - Triazole

U2 - 10.1016/j.bmcl.2008.04.080

DO - 10.1016/j.bmcl.2008.04.080

M3 - Article

C2 - 18513963

AN - SCOPUS:44649153722

SN - 0960-894X

VL - 18

SP - 3628

EP - 3631

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 12

ER -

Design, synthesis and evaluation of potent thymidylate synthase X inhibitors

Abstract

Keywords

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