Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A
template-based approach-Part 2.

J 2011

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2.

DWYER, Michael, Kamil PARUCH, Marc LABROLI, Carmen ALVAREZ, Kerry KEERTIKAR et. al.

Basic information

Original name

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2.

Name in Czech

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2.

Authors

DWYER, Michael (840 United States of America), Kamil PARUCH (203 Czech Republic, guarantor, belonging to the institution), Marc LABROLI (840 United States of America), Carmen ALVAREZ (840 United States of America), Kerry KEERTIKAR (840 United States of America), Cory POKER (840 United States of America), Randall ROSSMAN (840 United States of America), Thierry FISCHMANN (840 United States of America), Jose DUCA (840 United States of America), Vincent MADISON (840 United States of America), David PARRY (840 United States of America), Nicole DAVIS (840 United States of America), Wolfgang SEGHEZZI (840 United States of America), Derek WISWELL (840 United States of America) and Timothy GUZI (840 United States of America)

Edition

Bioorganic & Medicinal Chemistry Letters, Elsevier, 2011, 0960-894X

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

10401 Organic chemistry

Country of publisher

United States of America

Confidentiality degree

není předmětem státního či obchodního tajemství

Impact factor

Impact factor: 2.554

RIV identification code

RIV/00216224:14310/11:00055928

Organization unit

Faculty of Science

DOI

http://dx.doi.org/10.1016/j.bmcl.2010.10.113

UT WoS

000285544400097

Keywords in English

Kinase CHK1 Pyrazolo[1 5-a]pyrimidine Template

Abstract

V originále

Previous efforts by our group have established pyrazolo[1,5-a]pyrimidine as a viable core for the development of potent and selective CDK inhibitors. As part of an effort to utilize the pyrazolo[1,5-a]pyrimidine core as a template for the design and synthesis of potent and selective kinase inhibitors, we focused on a key regulator in the cell cycle progression, CHK1. Continued SAR development of the pyrazolo [1,5-a]pyrimidine core at the C5 and C6 positions, in conjunction with previously disclosed SAR at the C3 and C7 positions, led to the discovery of potent and selective CHK1 inhibitors.

Citovat

DWYER, Michael, Kamil PARUCH, Marc LABROLI, Carmen ALVAREZ, Kerry KEERTIKAR, Cory POKER, Randall ROSSMAN, Thierry FISCHMANN, Jose DUCA, Vincent MADISON, David PARRY, Nicole DAVIS, Wolfgang SEGHEZZI, Derek WISWELL and Timothy GUZI. Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2. Bioorganic & Medicinal Chemistry Letters. Elsevier, 2011, vol. 21, No 1, p. 471-474. ISSN 0960-894X. Available from: https://dx.doi.org/10.1016/j.bmcl.2010.10.113.

@article{974257,
   author = {Dwyer, Michael and Paruch, Kamil and Labroli, Marc and Alvarez, Carmen and Keertikar, Kerry and Poker, Cory and Rossman, Randall and Fischmann, Thierry and Duca, Jose and Madison, Vincent and Parry, David and Davis, Nicole and Seghezzi, Wolfgang and Wiswell, Derek and Guzi, Timothy},
   article_number = {1},
   doi = {http://dx.doi.org/10.1016/j.bmcl.2010.10.113},
   keywords = {Kinase CHK1 Pyrazolo[1 5-a]pyrimidine Template},
   language = {eng},
   issn = {0960-894X},
   journal = {Bioorganic & Medicinal Chemistry Letters},
   title = {Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2.},
   volume = {21},
   year = {2011}
}

TY  - JOUR
ID  - 974257
AU  - Dwyer, Michael - Paruch, Kamil - Labroli, Marc - Alvarez, Carmen - Keertikar, Kerry - Poker, Cory - Rossman, Randall - Fischmann, Thierry - Duca, Jose - Madison, Vincent - Parry, David - Davis, Nicole - Seghezzi, Wolfgang - Wiswell, Derek - Guzi, Timothy
PY  - 2011
TI  - Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2.
JF  - Bioorganic & Medicinal Chemistry Letters
VL  - 21
IS  - 1
SP  - 471-474
EP  - 471-474
PB  - Elsevier
SN  - 0960894X
KW  - Kinase CHK1 Pyrazolo[1 5-a]pyrimidine Template
N2  - Previous efforts by our group have established pyrazolo[1,5-a]pyrimidine as a viable core for the development of potent and selective CDK inhibitors. As part of an effort to utilize the pyrazolo[1,5-a]pyrimidine core as a template for the design and synthesis of potent and selective kinase inhibitors, we focused on a key regulator in the cell cycle progression, CHK1. Continued SAR development of the pyrazolo [1,5-a]pyrimidine core at the C5 and C6 positions, in conjunction with previously disclosed SAR at the C3 and C7 positions, led to the discovery of potent and selective CHK1 inhibitors.
ER  -

DWYER, Michael, Kamil PARUCH, Marc LABROLI, Carmen ALVAREZ, Kerry KEERTIKAR, Cory POKER, Randall ROSSMAN, Thierry FISCHMANN, Jose DUCA, Vincent MADISON, David PARRY, Nicole DAVIS, Wolfgang SEGHEZZI, Derek WISWELL and Timothy GUZI. Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2. \textit{Bioorganic \&{} Medicinal Chemistry Letters}. Elsevier, 2011, vol.~21, No~1, p.~471-474. ISSN~0960-894X. Available from: https://dx.doi.org/10.1016/j.bmcl.2010.10.113.

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