Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4,6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT. [PDF]
, 2018 FMS-like Tyrosine Kinase 3 (FLT3) is a clinically validated target for acute myeloid leukemia (AML). Inhibitors targeting FLT3 have been evaluated in clinical studies and have exhibited potential to treat FLT3-driven AML.
Bharate, Jaideep B +8 more
core +2 more sources
Iridium-Catalyzed Silylation of Five-Membered Heteroarenes: High Sterically Derived Selectivity from a Pyridyl-Imidazoline Ligand. [PDF]
, 2020 The steric effects of substituents on five-membered rings are less pronounced than those on six-membered rings because of the difference in bond angles. Thus, the regioselectivities of reactions of five-membered heteroarenes that occur with selectivities
Hartwig, John F +3 more
core +1 more source
Trispyrazolylborate Ligands Supported on Vinyl Addition Polynorbornenes and Their Copper Derivatives as Recyclable Catalysts [PDF]
, 2019 Polynorbornenes prepared by vinyl addition poly- merization and bearing pendant alkenyl groups serve as skeletons to support trispyrazolylborate ligands (Tpx) built at those alkenyl sites.
Albéniz Jiménez, Ana Carmen +6 more
core +2 more sources
Synthesis of pyrazole and pyrazole amidocobaloximes
, 2004 Department of Chemistry, Osmania University, Hyderabad-500 007, India E-mail : ssnsirasani @yahoo.com Manuscript received 23 September 2002, revised 23 April 2003. accepted 11 July 2003 A series of cyano (ligand) cobaloximes have been prepared where, the ligand is pyrazole (Pz), 1-(acetamido)pyrazole (Apz), 1-(N-methylacetamido)pyrazole (MAPz), 1 ...
A. Rajeshwar Rao +3 more
openaire +1 more source
The structure of the agrochemical fungicidal 4-Chloro-3-(3,5-dichloropheny)-1H-pyrazole, RPA 406194 and related compounds [PDF]
, 2003 The difficulties to obtain convenient monocrystals of the important fungicide RPA 406194 have been overcome by a combination of solid state 13C NMR, X-ray powder diffraction and molecular modeling.
Abboud +35 more
core +2 more sources
Inhibition of dengue virus replication by novel inhibitors of RNA-dependent RNA polymerase and protease activities [PDF]
, 2017 Dengue virus (DENV) is the leading mosquito-transmitted viral infection in the world. With more than 390 million new infections annually, and up to 1 million clinical cases with severe disease manifestations, there continues to be a need to develop new ...
Coluccia, A. +9 more
core +1 more source
Synthesis, biological evaluation, and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis: Part 2. Synthesis of rigid pyrazolones [PDF]
, 2009 Two series of novel rigid pyrazolone derivatives were synthesized and evaluated as inhibitors of Mycobacterium tuberculosis (MTB), the causative agent of tuberculosis. Two of these compounds showed a high activity against MTB (MIC = 4 μg/mL).
Alessandro De Logu +19 more
core +1 more source
Dizajniranje i sinteza novih derivata tiofenkarbohidrazida, tienopirazola i tienopirimidina s antioksidativnim i antitumorskim djelovanjem [PDF]
, 2010 2-Amino-5-acetyl-4-methyl-thiophene-3-carboxylic acid ethyl ester (1) and 5-acetyl-2-amino-4-methylthiophene-3-carbohydrazide (2) were synthesized and used as starting materials for the synthesis of new series of 1-(5-amino-4-(3,5-dimethyl-1H-pyrazole-1 ...
A. El-Gazzar +24 more
core +3 more sources
3‐Oxabicyclo[3.1.1]heptane as an Isostere of meta‐Benzene
Angewandte Chemie, EarlyView.3‐Oxabicyclo[3.1.1]heptanes were designed as saturated isosteres of meta‐benzene. Crystallographic analysis revealed that these structures and meta‐benzene have identical geometric properties. Replacement of the central benzene ring in the anticancer drug Sonidegib with 3‐oxabicyclo[3.1.1]heptane provided a patent‐free analogue with a nanomolar potency,
Dmitry Dibchak, Pavel K. Mykhailiuk
wiley +2 more sources