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 Flynn

Omar Morales, Yi Chen

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

16 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

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10.1016/j.bmcl.2005.12.092

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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 - https://www.scopus.com/pages/publications/33144460233

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

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