213416-36-5Relevant academic research and scientific papers
Synthesis and characterization of α-phosphorylated ketones: Models for the molybdopterin precursor
Van Houten, Kelly A.,Boggs, Christine M.,Pilato, Robert S.
, p. 10973 - 10986 (1998)
Synthesis of pyridyl substituted α-keto six membered cyclic phosphates is reported. These compounds are structurally similar to the precursor of molybdopterin (MPT), an important biological cofactor. We demonstrate that these α-phosphorylated ketones can undergo the fundamental transformation required for MFF synthesis.
OXADIAZOLE COMPOUNDS
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Paragraph 00372, (2019/12/04)
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
BENZIMIDAZOLONE DERIVED INHIBITORS OF BCL6
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Paragraph 00235, (2018/12/13)
The present invention relates to compounds of Formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: wherein X1, X2, R1, R2 and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.
Non-nucleosidic analogues of polyaminonucleosides and their influence on thermodynamic properties of derived oligonucleotides
Brzezinska, Jolanta,Markiewicz, Wojciech T.
, p. 12652 - 12669 (2015/08/18)
The rationale for the synthesis of cationic modified nucleosides is higher expected nuclease resistance and potentially better cellular uptake due to an overall reduced negative charge based on internal charge compensation. Due to the ideal distance between cationic groups, polyamines are perfect counterions for oligodeoxyribonucleotides. We have synthesized non-nucleosidic analogues built from units that carry different diol structures instead of sugar residues and functionalized with polyamines. The non-nucleosidic analogues were attached as internal or 5′-terminal modifications in oligodeoxyribonucleotide strands. The thermodynamic studies of these polyaminooligonucleotide analogues revealed stabilizing or destabilizing effects that depend on the linker or polyamine used.
Synthesis of 1′,2′-cis-Nucleoside analogues: Evidence of stereoelectronic control for SN2 reactions at the anomeric center of furanosides
Prevost, Michel,St-Jean, Olivier,Guindon, Yvan
supporting information; experimental part, p. 12433 - 12439 (2010/11/03)
We are reporting a highly diastereoselective route to 1′,2′- cis-nucleoside analogues in the d-ribo, d-lyxo, d-xylo, and d-arabinoside series. Five-membered ring lactols undergo highly selective N-glycosidation reactions in the presence of dimethylboron bromide with different silylated nucleobases. Stereoelectronic control plays a crucial role for the observed induction, and the products are proposed to be formed through SN2 "exploded" transition states. This approach shows great potential considering its simplicity and selectivity for the synthesis of nucleoside analogues, an important class of molecules in medicinal chemistry.
OXIM DERIVATIVES AS HSP90 INHIBITORS
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Page/Page column 221; 244, (2009/09/05)
The invention relates to HSP90 inhibiting compounds consisting of the formula: (I) wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
Cycloalkyl substituted polyamines for cancer therapy and methods of synthesis therefor
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Page/Page column 17-18, (2010/01/31)
Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
