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» Authors » Angeline C-H Lee

Angeline C-H Lee

Explore the profile of Angeline C-H Lee including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 6
Citations 96
Followers 0
Related Specialties
Chemistry
Biochemistry
Top 10 Co-Authors
Anthony D William
Anders Poulsen
Kee Chuan Goh
Eric T Sun
Stephanie Blanchard
Brian W Dymock
Ee Ling Teo
Kantharaj Ethirajulu
Meredith Williams
Jeanette M Wood
Published In
J Med Chem
Bioorg Med Chem Lett
Chimia (Aarau)
Affiliations
Soon will be listed here.
Recent Articles
1.
Acid Mediated Ring Closing Metathesis: A Powerful Synthetic Tool Enabling the Synthesis of Clinical Stage Kinase Inhibitors
William A, Lee A
Chimia (Aarau) . 2015 Oct; 69(3):142-5. PMID: 26507218
The powerful olefin metathesis reaction was employed for the construction of late-phase clinical agents SB1317 and SB1518. In both cases RCM seems to proceed only in the presence of an...
2.
Thieno[3,2-d]pyrimidin-4(3H)-one derivatives as PDK1 inhibitors discovered by fragment-based screening
Lee A, Ramanujulu P, Poulsen A, Williams M, Blanchard S, Ma D, et al.
Bioorg Med Chem Lett . 2012 May; 22(12):4023-7. PMID: 22591730
Ligand efficient fragments binding to PDK1 were identified by an NMR fragment-based screening approach. Computational modeling of the fragments bound to the active site led to the design and synthesis...
3.
Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine...
William A, Lee A, Poulsen A, Goh K, Madan B, Hart S, et al.
J Med Chem . 2012 Feb; 55(6):2623-40. PMID: 22339472
Herein, we describe the synthesis and SAR of a series of small molecule macrocycles that selectively inhibit JAK2 kinase within the JAK family and FLT3 kinase. Following a multiparameter optimization...
4.
Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs),...
William A, Lee A, Goh K, Blanchard S, Poulsen A, Teo E, et al.
J Med Chem . 2011 Dec; 55(1):169-96. PMID: 22148278
Herein, we describe the design, synthesis, and SAR of a series of unique small molecule macrocycles that show spectrum selective kinase inhibition of CDKs, JAK2, and FLT3. The most promising...
5.
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3)...
William A, Lee A, Blanchard S, Poulsen A, Teo E, Nagaraj H, et al.
J Med Chem . 2011 May; 54(13):4638-58. PMID: 21604762
Discovery of the activating mutation V617F in Janus Kinase 2 (JAK2(V617F)), a tyrosine kinase critically involved in receptor signaling, recently ignited interest in JAK2 inhibitor therapy as a treatment for...
6.
Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors
Blanchard S, William A, Lee A, Poulsen A, Teo E, Deng W, et al.
Bioorg Med Chem Lett . 2010 Mar; 20(8):2443-7. PMID: 20338758
A series of alkenyl indazoles were synthesized and evaluated in Aurora kinase enzyme assays. Several promising leads were optimized for selectivity towards Aurora B. Excellent binding affinity and good selectivity...