SYNTHESIS AND CYTOKININ-LIKE ACTIVITY OF 7-CHLORO-IMIDAZO-PYRIMIDINES
Some 5-amino substituted 7-chloro-imidazolpyrimidines and 7-chloro-8-methylthio-imidazopyrimidines were synthesized for further information on the role of the purine ring in cytokinin structure/activity relationships.Their cytokinin-like activity was examined using four different tests; expansion of cucumber etiolatedcotyledons; formation of chlorophyll in etiolated cotyledons of cucumber; preservation of chlorophyll breakdown in sections of barley leaves; inhibition of root growth in intact wheat seedlings.Compounds with imidazopyrimidine ring were generally less active than those with the purine ring, with the exception of the pentenylamino derivatives, which showed an activity comparable with that of the control, kinetin. Key Word Index--7-chloro-imidazopyrimidines; cytokinin activity; chlorophyll retention; leaf expansion; chlorophyll production; root growth inhibition.
Structure-based drug design of novel, potent, and selective azabenzimidazoles (ABI) as ATR inhibitors
Compound 13 was discovered through morphing of the ATR biochemical HTS hit 1. The ABI series was potent and selective for ATR. Incorporation of a 6-azaindole afforded a marked increase in cellular potency but was associated with poor PK and hERG ion channel inhibition. DMPK experiments established that CYP P450 and AO metabolism in conjunction with Pgp and BCRP efflux were major causative mechanisms for the observed PK. The series also harbored the CYP3A4 TDI liability driven by the presence of both a morpholine and an indole moiety. Incorporation of an adjacent fluorine or nitrogen into the 6-azaindole addressed many of the various medicinal chemistry issues encountered. (Chemical Presented).
Barsanti, Paul A.,Pan, Yue,Lu, Yipin,Jain, Rama,Cox, Matthew,Aversa, Robert J.,Dillon, Michael P.,Elling, Robert,Hu, Cheng,Jin, Xianming,Knapp, Mark,Lan, Jiong,Ramurthy, Savithri,Rudewicz, Patrick,Setti, Lina,Subramanian, Sharadha,Mathur, Michelle,Taricani, Lorena,Thomas, George,Xiao, Linda,Yue, Qin
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(2015/01/30)
SUBSTITUTED IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES
The invention relates to substituted imidazopyrimidines and triazolopyrimidines, to methods for the production thereof, and to the use of same for producing medicaments for the treatment and/or prophylaxis of diseases, especially haematological diseases, preferably leucopenia and neutropenia.
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(2010/05/13)
KINASE INHIBITORS
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(2010/10/20)
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