Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin

Carine Aubry; A. James Wilson; Paul R. Jenkins; Sachin Mahale; Bhabatosh Chaudhuri; Jean Didier Maréchal; Michael J. Sutcliffe

doi:10.1039/b518019h

Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin

Carine Aubry
, A. James Wilson
, Paul R. Jenkins
, Sachin Mahale
, Bhabatosh Chaudhuri
, Jean Didier Maréchal
, Michael J. Sutcliffe

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

Abstract

We present the design, synthesis, and biological activity of three classes of tryptamine derivatives, which are non-planar analogues of the toxic anti-cancer agent fascaplysin. We show these compounds to be selective inhibitors of CDK4 over CDK2, the most active compound 9q has an IC50 for the inhibition of CDK4 of 6 M. © The Royal Society of Chemistry 2006.

Original language	English
Pages (from-to)	787-801
Number of pages	14
Journal	Organic and Biomolecular Chemistry
Volume	4
Issue number	5
DOIs	https://doi.org/10.1039/b518019h
Publication status	Published - 2006

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10.1039/b518019h

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title = "Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin",

abstract = "We present the design, synthesis, and biological activity of three classes of tryptamine derivatives, which are non-planar analogues of the toxic anti-cancer agent fascaplysin. We show these compounds to be selective inhibitors of CDK4 over CDK2, the most active compound 9q has an IC50 for the inhibition of CDK4 of 6 M. {\textcopyright} The Royal Society of Chemistry 2006.",

author = "Carine Aubry and Wilson, \{A. James\} and Jenkins, \{Paul R.\} and Sachin Mahale and Bhabatosh Chaudhuri and Mar{\'e}chal, \{Jean Didier\} and Sutcliffe, \{Michael J.\}",

year = "2006",

doi = "10.1039/b518019h",

language = "English",

volume = "4",

pages = "787--801",

journal = "Organic and Biomolecular Chemistry",

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T1 - Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin

AU - Aubry, Carine

AU - Wilson, A. James

AU - Jenkins, Paul R.

AU - Mahale, Sachin

AU - Chaudhuri, Bhabatosh

AU - Maréchal, Jean Didier

AU - Sutcliffe, Michael J.

PY - 2006

Y1 - 2006

N2 - We present the design, synthesis, and biological activity of three classes of tryptamine derivatives, which are non-planar analogues of the toxic anti-cancer agent fascaplysin. We show these compounds to be selective inhibitors of CDK4 over CDK2, the most active compound 9q has an IC50 for the inhibition of CDK4 of 6 M. © The Royal Society of Chemistry 2006.

AB - We present the design, synthesis, and biological activity of three classes of tryptamine derivatives, which are non-planar analogues of the toxic anti-cancer agent fascaplysin. We show these compounds to be selective inhibitors of CDK4 over CDK2, the most active compound 9q has an IC50 for the inhibition of CDK4 of 6 M. © The Royal Society of Chemistry 2006.

U2 - 10.1039/b518019h

DO - 10.1039/b518019h

M3 - Article

SN - 1477-0520

VL - 4

SP - 787

EP - 801

JO - Organic and Biomolecular Chemistry

JF - Organic and Biomolecular Chemistry

IS - 5

ER -

Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin

Abstract

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