Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel antiproliferative agents: Exploration of core and headpiece structure–activity relationships
Dennis Powell
1
,
Ariamala Gopalsamy
1
,
Yanong Wang
1
,
Nan Zhang
1
,
Miriam Miranda
2
,
John P. McGinnis
2
,
Sridhar K. Rabindran
2
1
Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA
|
2
Oncology, Wyeth Research, Pearl River, NY 10965, USA
|
Publication type: Journal Article
Publication date: 2007-03-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
17275298
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
A novel series of antiproliferative agents containing pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides, selective for p21-deficient cells, were identified by high-throughput screening. Exploration of the SAR relationships in the headpiece, core, and tailpiece is described. Strict steric, positional, and electronic requirements were observed, with a clear preference for both core nitrogens, a thienoyl headpiece, and meta substituted tailpiece.
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Total citations:
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Citations from 2025:
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(3.23%)
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GOST
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Powell D. et al. Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel antiproliferative agents: Exploration of core and headpiece structure–activity relationships // Bioorganic and Medicinal Chemistry Letters. 2007. Vol. 17. No. 6. pp. 1641-1645.
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Powell D., Gopalsamy A., Wang Y., Zhang N., Miranda M., McGinnis J. P., Rabindran S. K. Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel antiproliferative agents: Exploration of core and headpiece structure–activity relationships // Bioorganic and Medicinal Chemistry Letters. 2007. Vol. 17. No. 6. pp. 1641-1645.
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RIS
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TY - JOUR
DO - 10.1016/j.bmcl.2006.12.116
UR - https://doi.org/10.1016/j.bmcl.2006.12.116
TI - Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel antiproliferative agents: Exploration of core and headpiece structure–activity relationships
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Powell, Dennis
AU - Gopalsamy, Ariamala
AU - Wang, Yanong
AU - Zhang, Nan
AU - Miranda, Miriam
AU - McGinnis, John P.
AU - Rabindran, Sridhar K.
PY - 2007
DA - 2007/03/01
PB - Elsevier
SP - 1641-1645
IS - 6
VL - 17
PMID - 17275298
SN - 0960-894X
SN - 1464-3405
ER -
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BibTex (up to 50 authors)
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@article{2007_Powell,
author = {Dennis Powell and Ariamala Gopalsamy and Yanong Wang and Nan Zhang and Miriam Miranda and John P. McGinnis and Sridhar K. Rabindran},
title = {Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel antiproliferative agents: Exploration of core and headpiece structure–activity relationships},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2007},
volume = {17},
publisher = {Elsevier},
month = {mar},
url = {https://doi.org/10.1016/j.bmcl.2006.12.116},
number = {6},
pages = {1641--1645},
doi = {10.1016/j.bmcl.2006.12.116}
}
Cite this
MLA
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Powell, Dennis, et al. “Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel antiproliferative agents: Exploration of core and headpiece structure–activity relationships.” Bioorganic and Medicinal Chemistry Letters, vol. 17, no. 6, Mar. 2007, pp. 1641-1645. https://doi.org/10.1016/j.bmcl.2006.12.116.