Discovery of Brivanib Alaninate ((S)-((R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), A …

…, S Mortillo, R Jeyaseelan Sr, DW Kukral… - Journal of medicinal …, 2008 - ACS Publications
A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 (BMS-540215)
was prepared in an effort to improve the aqueous solubility and oral bioavailability …

[HTML][HTML] Bruton's tyrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of …

…, EM Heimrich, KW McIntyre, TL Taylor, DW Kukral… - PloS one, 2017 - journals.plos.org
Bruton’s tyrosine kinase (BTK) regulates critical signal transduction pathways involved in the
pathobiology of rheumatoid arthritis (RA) and other autoimmune disorders. BMS-986142 is …

Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure–Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2 …

…, T Taylor, MA Pattoli, S Skala, DW Kukral… - Journal of Medicinal …, 2016 - ACS Publications
Bruton’s tyrosine kinase (BTK) belongs to the TEC family of nonreceptor tyrosine kinases and
plays a critical role in multiple cell types responsible for numerous autoimmune diseases. …

Design, Synthesis, and Evaluation of Orally Active 4-(2,4-Difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as Dual Vascular Endothelial …

…, S Mortillo, R Jeyaseelan, DW Kukral… - Journal of medicinal …, 2005 - ACS Publications
A series of substituted 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines
was identified as potent and selective inhibitors of the tyrosine kinase activity of the …

Discovery and Evaluation of N-Cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a Selective and Orally …

…, R Jeyaseelan, A Kamath, DW Kukral… - Journal of medicinal …, 2006 - ACS Publications
Substituted 3-((2-(pyridin-2-ylamino)thiazol-5-ylmethyl)amino)benzamides were identified
as potent and selective inhibitors of vascular endothelial growth factor receptor-2 (VEGFR-2) …

Periodic, partial inhibition of IκB kinase β-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis

…, H Booth-Lute, G Yang, P Davies, DW Kukral… - … of Pharmacology and …, 2009 - ASPET
We have previously shown that inhibitors of IκB kinase β (IKKβ), including 4(2′-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline
(BMS-345541), are efficacious against …

Discovery and Preclinical Studies of (R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an In …

…, S Mortillo, R Jeyaseelan, D Kukral… - Journal of medicinal …, 2006 - ACS Publications
A series of substituted 4-(4-fluoro-1H-indol-5-yloxy)pyrrolo[2,1-f][1,2,4]triazine-based
inhibitors of vascular endothelial growth factor receptor-2 kinase is reported. Structure−activity …

Synthesis and biologic evaluation of a novel 18F-labeled adnectin as a PET radioligand for imaging PD-L1 expression

…, M Wright, J Kim, A Pena, D Kukral… - Journal of Nuclear …, 2018 - Soc Nuclear Med
The programmed death protein (PD-1) and its ligand (PD-L1) play critical roles in a checkpoint
pathway cancer cells exploit to evade the immune system. A same-day PET imaging …

Synthesis of canine seromucoid before and after total hepatectomy

JC Kukral, RJ Pancner, J Louch… - American Journal of …, 1962 - journals.physiology.org
The incorporation rate of S 35 DL-methionine into the perchloric acid-soluble (seromucoid)
fraction of serum was studied in the same four dogs before and after a one-stage total …

[CITATION][C] Discovery of brivanib alaninate, a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase …

…, BS Wautlet, S Mortillo, R Jeyaseelan Sr, DW Kukral… - J. Med. Chem, 2008