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.

Základní údaje

Originální název

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

Název česky

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

Autoři

Vydání

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

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

10401 Organic chemistry

Stát vydavatele

Spojené státy

Utajení

není předmětem státního či obchodního tajemství

Impakt faktor

Impact factor: 2.554

Kód RIV

RIV/00216224:14310/11:00055928

Organizační jednotka

Přírodovědecká fakulta

DOI

https://doi.org/10.1016/j.bmcl.2010.10.113

UT WoS

000285544400097

Klíčová slova anglicky

Kinase CHK1 Pyrazolo[1 5-a]pyrimidine Template

Štítky

rivok, ZR

Změněno: 5. 3. 2012 11:30, Ing. Zdeňka Rašková

Anotace

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 a Timothy GUZI. Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2. Bioorganic & Medicinal Chemistry Letters. Elsevier, 2011, roč. 21, č. 1, s. 471-474. ISSN 0960-894X. Dostupné z: https://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 = {https://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 a 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, roč.~21, č.~1, s.~471-474. ISSN~0960-894X. Dostupné z: https://doi.org/10.1016/j.bmcl.2010.10.113.

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