99216-67-8Relevant academic research and scientific papers
Chiral enantiopure organosilane precursors for the synthesis of periodic mesoporous organosilicas
Cohen, Orit,Abu-Reziq, Raed,Gelman, Dmitri
, p. 1675 - 1685 (2017/11/17)
The manuscript describes synthesis of new chiral organosilica networks starting from modified readily available enantiopure substances such as sugars and amino acids. We report on the successful preparation of robust all-chiral organosilicas by polymerization of the homochiral monomers. When the homochiral organosilane monomers were polymerized in mixtures of polar organic solvents and water in the presence of hydrochloric acid or tetrabutylammonium fluoride as catalysts, mainly spherical microparticles were obtained due to emulsification of the hydrophobic monomers in these mixtures. Polycondensation of the chiral organosilanes in the presence of Pluronic P123 as a template produced ordered mesoporous networks. The new all-chiral materials were characterized by SEM, STEM, BET, SAXS, IR, NMR and TGA.
Modifications of flexible nonyl chain and nucleobase head group of (+)-erythro-9-(2′s-hydroxy-3′s-nonyl)adenine [(+)-EHNA] as adenosine deaminase inhibitors
Kandalkar, Sachin R.,Ramaiah, Parimi Atchuta,Joshi, Manoj,Wavhal, Atul,Waman, Yogesh,Raje, Amol A.,Tambe, Ashwini,Ansari, Shariq,De, Siddhartha,Palle, Venkata P.,Mookhtiar, Kasim A.,Deshpande, Anil M.,Barawkar, Dinesh A.
, p. 5799 - 5819 (2017/09/28)
A series of terminal nonyl chain and nucleobase modified analogues of (+)-EHNA (III) were synthesized and evaluated for their ability to inhibit adenosine deaminase (ADA). The constrained carbon analogues of (+)-EHNA, 7a-7h, 10a-c, 12, 13, 14 and 17a-c appeared very potent with Ki values in the low nanomolar range. Thio-analogues of (+)-EHNA 24a-e wherein 5′C of nonyl chain replaced by sulfur atom found to be less potent compared to (+)-EHNA. Docking of the representative compounds into the active site of ADA was performed to understand structure-activity relationships. Compounds 7a (Ki: 1.1 nM) 7b (Ki: 5.2 nM) and 26a (Ki: 5.9 nM) showed suitable balance of potency, microsomal stability and demonstrated better pharmacokinetic properties as compared to (+)-EHNA and therefore may have therapeutic potential for various inflammatory diseases, hypertension and cancer.
IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS
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Paragraph 0275; 0288; 0289, (2016/03/13)
The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, G, T, Y1, Y2, Y3, and Y4 are as defined herein.
IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS
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Paragraph 0218-0220; 0231-0233, (2015/02/25)
The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, G, T, Y1, Y2, Y3, and Y4 are as defined herein.
Structural requirements for the antiproliferative activity of pre-mRNA splicing inhibitor FR901464
Osman, Sami,Albert, Brian J.,Wang, Yanping,Li, Miaosheng,Czaicki, Nancy L.,Koide, Kazunori
supporting information; experimental part, p. 895 - 904 (2011/03/20)
FR901464, a natural product isolated from a bacterium source, activates a reporter gene, inhibits pre-mRNA splicing, and shows antitumor activity. We previously reported the development of a more potent analogue, meayamycin, through the total synthesis of
FR901464 AND ANALOGS WITH ANTITUMOR ACTIVITY AND METHOD FOR THEIR PREPARATION
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Page/Page column 63, (2009/04/25)
The present invention provides analogs of FR901464, as well as a methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associated with dysfunctional RNA splicing.
SYNTHESIS OF FR901464 AND ANALOGS WITH ANTITUMOR ACTIVITY
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Page/Page column 27, (2008/06/13)
The present invention provides novel analogs of FR901464, as well as an improved methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associ
Diastereoselective synthesis of the acyl side-chain and amino acid (2S,3R)-3-hydroxy-3-methylproline fragments of polyoxypeptin A
Chen, Zhiyong,Ye, Tao
, p. 2781 - 2785 (2007/10/03)
Synthesis of the acyl side-chain and amino acid (2S,3R)-3-hydroxy-3- methylproline units of the potent depsipeptide polyoxypeptin A, is described. Key intermediates were secured via diastereoselective addition involving a homoenolate ion and allylation of
Dehydrooligopeptides. XVII. Practical syntheses of all of the diastereomers of N,N-protected 2,3-diaminobutanoic acids from L- and D-threonine derivatives
Nakamura,Hirai,Tamotsu,Yonezawa,Shin
, p. 1369 - 1377 (2007/10/02)
Syntheses of all of the dioctereomers of 2,3-diaminobutanoic acids, found in some pedtide antibiotics and toxins, were accomplished. The four isomers were derived mainly through two pathways including S(N)2 inversions of the β-substituent of L- or D-threonine derivatives. The various protecting groups and effective nucleophiles for the S(N)2 inversion were examined.
Facile Syntheses of (S,S)-2,3-Diaminobutyric Acid and Acid Containg N-Terminal Tripeptide of Antrimycins
Nakamura, Yutaka,Shin, Chung-gi
, p. 49 - 52 (2007/10/02)
The stereoselective synthesis of (S,S)-2,3-diaminobutyric acid (Dab), which is one of the four uncommon α-amino acid residues of antrimycins (1a) and cirratiomycins (1b), was accomplished.Furthermore, N-terminal tripeptide segment of 1 containing Dab resi
