75760-11-1Relevant academic research and scientific papers
ALPHA-5 BETA-1 INHIBITORS
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Paragraph 0323; 0325-0328, (2021/06/11)
The disclosure provides, inter alia, alpha-5 beta-1 inhibitors, pharmaceutical compositions comprising alpha-5 beta-1 inhibitors, methods for treating diseases using alpha-5 beta-1 inhibitors, and processes for making alpha-5 beta-1 inhibitors.
Design and synthesis of Fmoc-SPPS-ready iodoarene amino acid pre-catalysts and their reactivity in the catalytic oxytosylation of ketones
Brummel, Beau R.,Giambalvo, Lauren N.,Gross, Kristopher G.,Kobra, Khadijatul,Lex, Timothy R.,McMillen, Colin D.,Panda, Soham,Pennington, William T.,Swasy, Maria I.,Whitehead, Daniel C.
supporting information, (2020/02/22)
A small suite of iodo-aryl amide containing amino acids were synthesized and assessed as catalysts for the hypervalent iodine(III) mediated α-oxytosylation of ketones. The efficiency of each catalyst was determined by comparing the relative rates of catalysis in the direct α-oxytosylation of propiophenone. In addition, these catalysts can be easily converted to congeners that are suitable for Fmoc-solid phase peptide synthesis for facile incorporation into a chiral peptide framework. This work facilitates the broader goal of our program to develop peptide-based enantioselective catalysts for hypervalent iodine chemistry.
Functional Disruption of the Cancer-Relevant Interaction between Survivin and Histone H3 with a Guanidiniocarbonyl Pyrrole Ligand
Aschmann, Dennis,Bayer, Peter,Beuck, Christine,Ehlers, Martin,Giese, Michael,Killa, Matthias,Knauer, Shirley K.,Meiners, Annika,Mertel, Marcel,Schmuck, Carsten,Vallet, Cecilia
supporting information, p. 5567 - 5571 (2020/02/04)
The protein Survivin is highly upregulated in most cancers and considered to be a key player in carcinogenesis. We explored a supramolecular approach to address Survivin as a drug target by inhibiting the protein–protein interaction of Survivin and its fu
TRICYCLIC COMPOUNDS
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Paragraph 0610; 0611; 0612, (2014/06/25)
The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Highly enantioselective synthesis of orthogonally protected (2S)-2,3-diaminopropanoates through catalytic phase-transfer aza-Henry reaction
Kumaraswamy, Gullapalli,Pitchaiah, Arigala
, p. 1543 - 1550 (2011/10/08)
The syntheses of enantiomer-enriched orthogonally protected different (2S)-2,3-diaminopropanoates and unnatural furyl-substituted (tert-butoxy) carbonyl (Boc) as well as (benzyloxy)carbonyl (Cbz) protected amino acid esters are accomplished by means of an
Novel inhibitors of the αvβ3 integrin-lead identification strategy
Elliot, David,Henshaw, Eleanor,MacFaul, Philip A.,Morley, Andrew D.,Newham, Peter,Oldham, Keith,Page, Ken,Rankine, Neil,Sharpe, Paul,Ting, Attilla,Wood, Christine M.
scheme or table, p. 4832 - 4835 (2010/04/29)
A novel approach to inhibition of the αvβ3 integrin is described, which uses compounds designed to generate nM potency without using the arginine binding site.
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists
Palucki, Brenda L.,Park, Min K.,Nargund, Ravi P.,Tang, Rui,MacNeil, Tanya,Weinberg, David H.,Vongs, Aurawan,Rosenblum, Charles I.,Doss, George A.,Miller, Randall R.,Stearns, Ralph A.,Peng, Qianping,Tamvakopoulos, Constantin,Van Der Ploeg, Lex H. T.,Patchett, Arthur A.
, p. 1993 - 1996 (2007/10/03)
We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. The 5- and 6-alkylated piperazine compounds exhibit low bioactivation potential as measured by covale
Inhibitors of farnesyl-protein transferase
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, (2008/06/13)
The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl-protein transferase. Furthermore, these CAAX analogues differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
Inhibitors of farnesyl-protein transferase
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, (2008/06/13)
The present invention comprises analogs of the CA1 A2 X motif of the protein Ras that is modified by farnesylation in vivo. These CA1 A2 X analogs inhibit the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, these CA1 A2 X analogs differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. The compounds of the instant invention also incorporate a cyclic amine moiety in the A2 position of the motif. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
Nonpeptide glycoprotein IIb/IIIa inhibitors. 13. Design and synthesis of an orally active pyrazolopiperazinone nonpeptide fibrinogen receptor antagonist
Askew,McIntyre,Hunt,Claremon,Baldwin,Anderson,Gould,Lynch,Chang,Cook,Lynch,Holahan,Sitko,Stranieri
, p. 1531 - 1536 (2007/10/03)
The synthesis and antiplatelet activity of a series of pyrazolopiperazinone nonpeptide fibrinogen receptor antagonists is reported. The sulfonamide analog 6 (L-734,115), significantly inhibited ex vivo platelet aggregation 24 h after oral administration at doses of 1.0 and 2.0 mg/kg to dogs and rhesus monkeys, respectively.
