<i>tert</i>
            ‐Butylamine

Campbell, Kenneth N.; Sommers, Armiger H.; Campbell, Barbara K.; Smith, Lee Irvin; Emerson, Oliver H.; Pearson, D. E.; Baxter, John F.; Carter, K. N.

doi:10.1002/0471264180.os027.06

Organic Syntheses 2003

DOI: 10.1002/0471264180.os027.06

|View full text |Cite

tert ‐Butylamine

Kenneth N. Campbell¹,

Armiger H. Sommers²,

Barbara K. Campbell³

et al.

Abstract: tert ‐Butylamine intermediate: 2,2‐Dimethylethylenimine product: tert ‐butylamine intermediate: tert ‐butylurea solvent: 500 ml. of petroleum ether … Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2022

Publication Types

Select...

Article1

Relationship

Self Cite0

Independent1

Authors

Journals

Cited by 1 publication

(1 citation statement)

References 12 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Found: C, 55.49; H, 5.13; N, 23.81.5-(2-Hydroxyprop-1-yl)amino-3-isopropyl-7-[4-(pyrazol-1-yl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidin (4). 7-[4-(Pyrazol-1yl)benzyl]amino-3-isopropyl-5-methylsulfonyl-7-[4-(pyrazol-1-yl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine 3 (70 mg, 0.17 mmol)26 and (R/S)-1-amino-2-propanol (2 mL, 25 mmol) were heated in sealed ampule for 4 h at 150 °C. Excess amine was evaporated at a temperature below 60 °C, and the residue was partitioned in CHCl 3 /H 2 O.…”

mentioning

confidence: 99%

3,5,7-Substituted Pyrazolo[4,3-d]Pyrimidine Inhibitors of Cyclin-Dependent Kinases and Cyclin K Degraders

et al. 2022

View full text Add to dashboard Cite

3,5,7-Trisubstituted pyrazolo[4,3-d]pyrimidines have been identified as potent inhibitors of cyclin-dependent kinases (CDKs), which are established drug targets. Herein, we describe their further structural modifications leading to novel nanomolar inhibitors with strong antiproliferative activity. We determined the crystal structure of fully active CDK2/A2 with 5-(2-amino-1-ethyl)thio-3-cyclobutyl-7-[4-(pyrazol-1-yl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine (24) at 1.7 Å resolution, confirming the competitive mode of inhibition. Biochemical and cellular assays in lymphoma cell lines confirmed the expected mechanism of action through dephosphorylation of retinoblastoma protein and RNA polymerase II, leading to induction of apoptosis. Importantly, we also revealed an interesting ability of compound 24 to induce proteasome-dependent degradation of cyclin K both in vitro and in a patient-derived xenograft in vivo. We propose that 24 has a dual mechanism of action, acting as a kinase inhibitor and as a molecular glue inducing an interaction between CDK12 and DDB1 that leads to polyubiquitination of cyclin K and its subsequent degradation.

show abstract

mentioning

confidence: 99%

3,5,7-Substituted Pyrazolo[4,3-d]Pyrimidine Inhibitors of Cyclin-Dependent Kinases and Cyclin K Degraders

et al. 2022

View full text Add to dashboard Cite

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

tert ‐Butylamine

Abstract: tert ‐Butylamine intermediate: 2,2‐Dimethylethylenimine product: tert ‐butylamine intermediate: tert ‐butylurea solvent: 500 ml. of petroleum ether … Show more

Cited by 1 publication

References 12 publications

3,5,7-Substituted Pyrazolo[4,3-d]Pyrimidine Inhibitors of Cyclin-Dependent Kinases and Cyclin K Degraders

3,5,7-Substituted Pyrazolo[4,3-d]Pyrimidine Inhibitors of Cyclin-Dependent Kinases and Cyclin K Degraders

Contact Info

Product

Resources

About