3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2

George S. Sheppard; Jieyi Wang; Megumi Kawai; Nwe Y. BaMaung; Richard A. Craig; Scott A. Erickson; Linda Lynch; Jyoti Patel; Fan Yang; Xenia B. Searle; Pingping Lou; Chang Park; Ki H. Kim; Jack Henkin; Richard Lesniewski

doi:10.1016/j.bmcl.2003.12.031

3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2

George S. Sheppard^*, Jieyi Wang, Megumi Kawai, Nwe Y. BaMaung, Richard A. Craig, Scott A. Erickson, Linda Lynch, Jyoti Patel, Fan Yang, Xenia B. Searle, Pingping Lou, Chang Park, Ki H. Kim, Jack Henkin, Richard Lesniewski

^*Corresponding author for this work

CLP - Chemistry of Life Processes Institute

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

50 Scopus citations

Abstract

Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allowed the identification of potent inhibitors with good selectivity against MetAP1. Diacylhydrazine 3t (A-357300) was identified as an analogue displaying inhibition of methionine processing and cellular proliferation in human microvascular endothelial cells (HMVEC).

Original language	English (US)
Pages (from-to)	865-868
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	4
DOIs	https://doi.org/10.1016/j.bmcl.2003.12.031
State	Published - Feb 23 2004

ASJC Scopus subject areas

Drug Discovery
Molecular Medicine
Molecular Biology
Biochemistry
Clinical Biochemistry
Pharmaceutical Science
Organic Chemistry

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10.1016/j.bmcl.2003.12.031

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Sheppard, G. S., Wang, J., Kawai, M., BaMaung, N. Y., Craig, R. A., Erickson, S. A., Lynch, L., Patel, J., Yang, F., Searle, X. B., Lou, P., Park, C., Kim, K. H., Henkin, J., & Lesniewski, R. (2004). 3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2. Bioorganic and Medicinal Chemistry Letters, 14(4), 865-868. https://doi.org/10.1016/j.bmcl.2003.12.031

@article{a1acb744c96a4318be4dbf9befdd60de,

title = "3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2",

abstract = "Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allowed the identification of potent inhibitors with good selectivity against MetAP1. Diacylhydrazine 3t (A-357300) was identified as an analogue displaying inhibition of methionine processing and cellular proliferation in human microvascular endothelial cells (HMVEC).",

author = "Sheppard, {George S.} and Jieyi Wang and Megumi Kawai and BaMaung, {Nwe Y.} and Craig, {Richard A.} and Erickson, {Scott A.} and Linda Lynch and Jyoti Patel and Fan Yang and Searle, {Xenia B.} and Pingping Lou and Chang Park and Kim, {Ki H.} and Jack Henkin and Richard Lesniewski",

year = "2004",

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doi = "10.1016/j.bmcl.2003.12.031",

language = "English (US)",

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Sheppard, GS, Wang, J, Kawai, M, BaMaung, NY, Craig, RA, Erickson, SA, Lynch, L, Patel, J, Yang, F, Searle, XB, Lou, P, Park, C, Kim, KH, Henkin, J & Lesniewski, R 2004, '3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2', Bioorganic and Medicinal Chemistry Letters, vol. 14, no. 4, pp. 865-868. https://doi.org/10.1016/j.bmcl.2003.12.031

TY - JOUR

T1 - 3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2

AU - Sheppard, George S.

AU - Wang, Jieyi

AU - Kawai, Megumi

AU - BaMaung, Nwe Y.

AU - Craig, Richard A.

AU - Erickson, Scott A.

AU - Lynch, Linda

AU - Patel, Jyoti

AU - Yang, Fan

AU - Searle, Xenia B.

AU - Lou, Pingping

AU - Park, Chang

AU - Kim, Ki H.

AU - Henkin, Jack

AU - Lesniewski, Richard

PY - 2004/2/23

Y1 - 2004/2/23

N2 - Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allowed the identification of potent inhibitors with good selectivity against MetAP1. Diacylhydrazine 3t (A-357300) was identified as an analogue displaying inhibition of methionine processing and cellular proliferation in human microvascular endothelial cells (HMVEC).

AB - Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allowed the identification of potent inhibitors with good selectivity against MetAP1. Diacylhydrazine 3t (A-357300) was identified as an analogue displaying inhibition of methionine processing and cellular proliferation in human microvascular endothelial cells (HMVEC).

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U2 - 10.1016/j.bmcl.2003.12.031

DO - 10.1016/j.bmcl.2003.12.031

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AN - SCOPUS:10744228072

SN - 0960-894X

VL - 14

SP - 865

EP - 868

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 4

ER -

3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2

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