Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 1.

Bénédicte Delouvrié; Katherine Al-Kadhimi; Jean-Claude Arnould; Simon T Barry; Darren A E Cross; Myriam Didelot; Paul R Gavine; Hervé Germain; Craig S Harris; Adina M Hughes; David A Jude; Jane Kendrew; Christine Lambert-van der Brempt; Jean-Jacques Lohmann; Morgan Ménard; Andrew A Mortlock; Martin Pass; Claire Rooney; Michel Vautier; Jennifer L Vincent; Nicolas Warin

doi:10.1016/j.bmcl.2012.04.063

Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 1.

Bénédicte Delouvrié, Katherine Al-Kadhimi, Jean-Claude Arnould, Simon T Barry, Darren A E Cross, Myriam Didelot, Paul R Gavine, Hervé Germain, Craig S Harris, Adina M Hughes, David A Jude, Jane Kendrew, Christine Lambert-van der Brempt, Jean-Jacques Lohmann, Morgan Ménard, Andrew A Mortlock, Martin Pass, Claire Rooney, Michel Vautier, Jennifer L VincentNicolas Warin

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

Abstract

Potent antagonists of the integrin α(5)β(1), which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker between the basic group and the phenyl central core.

Original language	English
Journal	Bioorganic & medicinal chemistry letters
Volume	22
Issue number	12
DOIs	https://doi.org/10.1016/j.bmcl.2012.04.063
Publication status	Published - 15 Jun 2012

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10.1016/j.bmcl.2012.04.063

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Delouvrié, B., Al-Kadhimi, K., Arnould, J.-C., Barry, S. T., Cross, D. A. E., Didelot, M., Gavine, P. R., Germain, H., Harris, C. S., Hughes, A. M., Jude, D. A., Kendrew, J., Lambert-van der Brempt, C., Lohmann, J.-J., Ménard, M., Mortlock, A. A., Pass, M., Rooney, C., Vautier, M., ... Warin, N. (2012). Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 1. Bioorganic & medicinal chemistry letters, 22(12). https://doi.org/10.1016/j.bmcl.2012.04.063

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title = "Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 1.",

abstract = "Potent antagonists of the integrin α(5)β(1), which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker between the basic group and the phenyl central core.",

author = "B{\'e}n{\'e}dicte Delouvri{\'e} and Katherine Al-Kadhimi and Jean-Claude Arnould and Barry, {Simon T} and Cross, {Darren A E} and Myriam Didelot and Gavine, {Paul R} and Herv{\'e} Germain and Harris, {Craig S} and Hughes, {Adina M} and Jude, {David A} and Jane Kendrew and {Lambert-van der Brempt}, Christine and Jean-Jacques Lohmann and Morgan M{\'e}nard and Mortlock, {Andrew A} and Martin Pass and Claire Rooney and Michel Vautier and Vincent, {Jennifer L} and Nicolas Warin",

year = "2012",

month = jun,

day = "15",

doi = "10.1016/j.bmcl.2012.04.063",

language = "English",

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journal = "Bioorganic & medicinal chemistry letters",

issn = "1464-3405",

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Delouvrié, B, Al-Kadhimi, K, Arnould, J-C, Barry, ST, Cross, DAE, Didelot, M, Gavine, PR, Germain, H, Harris, CS, Hughes, AM, Jude, DA, Kendrew, J, Lambert-van der Brempt, C, Lohmann, J-J, Ménard, M, Mortlock, AA, Pass, M, Rooney, C, Vautier, M, Vincent, JL & Warin, N 2012, 'Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 1.', Bioorganic & medicinal chemistry letters, vol. 22, no. 12. https://doi.org/10.1016/j.bmcl.2012.04.063

TY - JOUR

T1 - Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 1.

AU - Delouvrié, Bénédicte

AU - Al-Kadhimi, Katherine

AU - Arnould, Jean-Claude

AU - Barry, Simon T

AU - Cross, Darren A E

AU - Didelot, Myriam

AU - Gavine, Paul R

AU - Germain, Hervé

AU - Harris, Craig S

AU - Hughes, Adina M

AU - Jude, David A

AU - Kendrew, Jane

AU - Lambert-van der Brempt, Christine

AU - Lohmann, Jean-Jacques

AU - Ménard, Morgan

AU - Mortlock, Andrew A

AU - Pass, Martin

AU - Rooney, Claire

AU - Vautier, Michel

AU - Vincent, Jennifer L

AU - Warin, Nicolas

PY - 2012/6/15

Y1 - 2012/6/15

N2 - Potent antagonists of the integrin α(5)β(1), which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker between the basic group and the phenyl central core.

AB - Potent antagonists of the integrin α(5)β(1), which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker between the basic group and the phenyl central core.

U2 - 10.1016/j.bmcl.2012.04.063

DO - 10.1016/j.bmcl.2012.04.063

M3 - Article

C2 - 22575869

SN - 1464-3405

VL - 22

JO - Bioorganic & medicinal chemistry letters

JF - Bioorganic & medicinal chemistry letters

IS - 12

ER -

Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 1.

Abstract

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