Oza, Vibha published the artcileSynthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors, Computed Properties of 763120-58-7, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(6), 2330-2337, database is CAplus and MEDLINE.
Checkpoint kinase 1 (Chk1, CHEK1) is a Ser/Thr protein kinase that plays a key role in mediating the cellular response to DNA damage. Synthesis and evaluation of a previously described class of Chk1 inhibitors, triazoloquinolones/triazolones (TZs) is further described. Investigation of structure-activity relationships led to the identification of potent inhibitors I [R1 = 2-thienyl, 2-pyrrolyl, R2 = NH2; R1 = 2-pyrrolyl, R2 = CH2OH (II)]. Key challenges included modulation of physicochem. properties and pharmacokinetic parameters to enable compound testing in a Chk1 specific hollow fiber pharmacodynamic model. In this model, II was shown to abrogate topotecan-induced cell cycle arrest in a dose dependent manner. The demonstrated activity of TZs in this model in combination with a chemotherapeutic agent as well as radiotherapy validates this series of Chk1 inhibitors. X-ray crystal structures for an initial lead and an optimized analog are also presented.
Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Computed Properties of 763120-58-7.
Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics