117401-78-2

Upstream product

• 619-25-0 3-Nitrobenzyl alcohol 
• 117401-73-7 1-allyloxymethyl-3-nitrobenzene 

Downstream Products

• 144161-22-8 m-azidobenzyl allyl ether 
• 1354567-52-4 (4-{3-[(allylmethylamino)methyl]phenyl}pyrimidin-2-yl)-(3-allyloxymethylphenyl)amine 
• 1364123-95-4 (3-allyloxymethylphenyl)-[4-(5-allyloxymethylpyridin-3-yl)pyrimidin-2-yl]amine 
• 1364123-93-2 [4-(5-allyloxymethylfuran-2-yl)pyrimidin-2-yl]-(3-allyloxymethylphenyl)amine 
• 1364123-94-3 [4-(1-allyl-1H-indol-6-yl)pyrimidin-2-yl]-(3-allyloxymethylphenyl)amine 
• 937273-27-3 (3-allyloxymethyl-phenyl)-[4-(3-but-3-enyloxy-phenyl)-pyrimidin-2-yl]-amine 
• 144117-74-8 N-<(6-m-azidobenzyloxy)-E,E-2,4-hexadienoamide>-L-tyrosyl-N,N'-di-Boc-spermine-N-α-N^G,N^G'-tri-Boc-L-arginine di-amide 
• 144117-78-2 N-((6-m-azidobenzyloxy)-E,E-2,4-hexadienoamide)-L-tyrosyl-N,N'-di-Boc-spermine-N_α,N_ε-di-Boc-L-lysine di-amide 
• 144117-73-7 6-(m-azidobenzyloxy)-E,E-2,4-hexadienoic acid N-hydroxysuccinimide ester 
• 144117-71-5 ethyl-6-(m-azidobenzyloxy)-E,E-2,4-hexadienoate 
• 144117-72-6 6-(m-azidobenzyloxy)-E,E-2,4-hexadienoic acid 
• 144136-92-5 2-(m-azidobenzyloxy)-acetaldehyde 

Relevant academic research and scientific papers

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), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer

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 leads were assessed in vitro for their inhibition of cancer cell proliferation, solubility, CYP450 inhibition, and microsomal stability. This screening cascade revealed 26h as a preferred compound with target IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively. Pharmacokinetic (PK) studies of 26h in preclinical species showed good oral exposures. Oral efficacy was observed in colon (HCT-116) and lymphoma (Ramos) xenograft studies, in line with the observed PK/PD correlation. 26h (SB1317/TG02) was progressed into development in 2010 and is currently undergoing phase 1 clinical trials in advanced leukemias and multiple myeloma.

Discovery of the macrocycle (9 E)-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-liketyrosine kinase-3 (J

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 of a key aryl ring of the previously described SB1518 (

OXYGEN LINKED PYRIMIDINE DERIVATIVES

The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.

Synthesis of novel and photolabile philanthotoxin analogs: Glutamate receptor antagonists

The synthetic methods for 27 novel and photolabile philanthotoxin analogs are described. Most analogs were synthesized by two general methods with modifications of these methods where necessary.