Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis

Lee A. McDermott; Brian Higgins; Mary Simcox; Kin Chun Luk; Tom Nevins; Kenneth Kolinsky; Melissa Smith; Hong Yang; Jia K. Li; Yingsi Chen; June Ke; Navita Mallalieu; Tom Egan; Stan Kolis; Aruna Railkar; Louise Gerber; Jin Jun Liu; Fred Konzelmann; Zhuming Zhang; Tom Flynn; Omar Morales; Yi Chen

doi:10.1016/j.bmcl.2005.12.092

Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis

Lee A. McDermott, Brian Higgins, Mary Simcox, Kin Chun Luk, Tom Nevins, Kenneth Kolinsky, Melissa Smith, Hong Yang, Jia K. Li, Yingsi Chen, June Ke, Navita Mallalieu, Tom Egan, Stan Kolis, Aruna Railkar, Louise Gerber, Jin Jun Liu, Fred Konzelmann, Zhuming Zhang, Tom FlynnOmar Morales, Yi Chen

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

14 Scopus citations

Abstract

RO4396686 is a small molecule KDR, FGFR, and PDGFR inhibitor with good pharmacokinetic properties in rodents. In a mouse corneal neovascularization assay, this compound inhibited VEGF-induced angiogenesis. Tested in a H460a xenograft tumor model this agent effected significant tumor growth inhibition at doses as low as 50 mg/kg.

Original language	English
Pages (from-to)	1950-1953
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2005.12.092
State	Published - 1 Apr 2006
Externally published	Yes

Keywords

Biological results
FGFR
Inhibitor
KDR
PDGFR
Pyrimidopyrimidone

Access to Document

10.1016/j.bmcl.2005.12.092

Cite this

McDermott, L. A., Higgins, B., Simcox, M., Luk, K. C., Nevins, T., Kolinsky, K., Smith, M., Yang, H., Li, J. K., Chen, Y., Ke, J., Mallalieu, N., Egan, T., Kolis, S., Railkar, A., Gerber, L., Liu, J. J., Konzelmann, F., Zhang, Z., ... Chen, Y. (2006). Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorganic and Medicinal Chemistry Letters, 16(7), 1950-1953. https://doi.org/10.1016/j.bmcl.2005.12.092

@article{968736af612b45808f8872e4d438e91d,

title = "Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis",

abstract = "RO4396686 is a small molecule KDR, FGFR, and PDGFR inhibitor with good pharmacokinetic properties in rodents. In a mouse corneal neovascularization assay, this compound inhibited VEGF-induced angiogenesis. Tested in a H460a xenograft tumor model this agent effected significant tumor growth inhibition at doses as low as 50 mg/kg.",

keywords = "Biological results, FGFR, Inhibitor, KDR, PDGFR, Pyrimidopyrimidone",

author = "McDermott, {Lee A.} and Brian Higgins and Mary Simcox and Luk, {Kin Chun} and Tom Nevins and Kenneth Kolinsky and Melissa Smith and Hong Yang and Li, {Jia K.} and Yingsi Chen and June Ke and Navita Mallalieu and Tom Egan and Stan Kolis and Aruna Railkar and Louise Gerber and Liu, {Jin Jun} and Fred Konzelmann and Zhuming Zhang and Tom Flynn and Omar Morales and Yi Chen",

year = "2006",

month = apr,

day = "1",

doi = "10.1016/j.bmcl.2005.12.092",

language = "English",

volume = "16",

pages = "1950--1953",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

number = "7",

}

McDermott, LA, Higgins, B, Simcox, M, Luk, KC, Nevins, T, Kolinsky, K, Smith, M, Yang, H, Li, JK, Chen, Y, Ke, J, Mallalieu, N, Egan, T, Kolis, S, Railkar, A, Gerber, L, Liu, JJ, Konzelmann, F, Zhang, Z, Flynn, T, Morales, O & Chen, Y 2006, 'Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis', Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 7, pp. 1950-1953. https://doi.org/10.1016/j.bmcl.2005.12.092

TY - JOUR

T1 - Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis

AU - McDermott, Lee A.

AU - Higgins, Brian

AU - Simcox, Mary

AU - Luk, Kin Chun

AU - Nevins, Tom

AU - Kolinsky, Kenneth

AU - Smith, Melissa

AU - Yang, Hong

AU - Li, Jia K.

AU - Chen, Yingsi

AU - Ke, June

AU - Mallalieu, Navita

AU - Egan, Tom

AU - Kolis, Stan

AU - Railkar, Aruna

AU - Gerber, Louise

AU - Liu, Jin Jun

AU - Konzelmann, Fred

AU - Zhang, Zhuming

AU - Flynn, Tom

AU - Morales, Omar

AU - Chen, Yi

PY - 2006/4/1

Y1 - 2006/4/1

N2 - RO4396686 is a small molecule KDR, FGFR, and PDGFR inhibitor with good pharmacokinetic properties in rodents. In a mouse corneal neovascularization assay, this compound inhibited VEGF-induced angiogenesis. Tested in a H460a xenograft tumor model this agent effected significant tumor growth inhibition at doses as low as 50 mg/kg.

AB - RO4396686 is a small molecule KDR, FGFR, and PDGFR inhibitor with good pharmacokinetic properties in rodents. In a mouse corneal neovascularization assay, this compound inhibited VEGF-induced angiogenesis. Tested in a H460a xenograft tumor model this agent effected significant tumor growth inhibition at doses as low as 50 mg/kg.

KW - Biological results

KW - FGFR

KW - Inhibitor

KW - KDR

KW - PDGFR

KW - Pyrimidopyrimidone

UR - http://www.scopus.com/inward/record.url?scp=33144460233&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2005.12.092

DO - 10.1016/j.bmcl.2005.12.092

M3 - Article

C2 - 16460940

AN - SCOPUS:33144460233

SN - 0960-894X

VL - 16

SP - 1950

EP - 1953

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 7

ER -

Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis

Abstract

Keywords

Access to Document

Fingerprint

Cite this