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» Authors » Rajeev S Bhide

Rajeev S Bhide

Explore the profile of Rajeev S Bhide including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 18
Citations 166
Followers 0
Related Specialties
Biochemistry
Chemistry
Pharmacology
Top 10 Co-Authors
John T Hunt
Louis J Lombardo
Ligang Qian
Joseph Fargnoli
Zhen-Wei Cai
Robert Jeyaseelan Sr
Joel C Barrish
Robert M Borzilleri
Amrita Kamath
Michael A Poss
Published In
Bioorg Med Chem Lett
J Med Chem
Org Lett
Drug Metab Dispos
Mol Cancer Ther
Affiliations
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Recent Articles
1.
Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis
Nair S, Kumar S, Paidi V, Sistla R, Kantheti D, Polimera S, et al.
ACS Med Chem Lett . 2020 Jul; 11(7):1402-1409. PMID: 32676146
IRAK4 is an attractive therapeutic target for the treatment of inflammatory conditions. Structure guided optimization of a nicotinamide series of inhibitors has been expanded to explore the IRAK4 front pocket....
2.
Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors
Bhide R, Keon A, Weigelt C, Sack J, Schmidt R, Lin S, et al.
Bioorg Med Chem Lett . 2017 Sep; 27(21):4908-4913. PMID: 28947151
The identification of small molecule inhibitors of IRAK4 for the treatment of autoimmune diseases has been an area of intense research. We discovered novel 4,6-diaminonicotinamides which potently inhibit IRAK4. Optimization...
3.
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders
Liu Q, Shi Q, Marcoux D, Batt D, Cornelius L, Qin L, et al.
J Med Chem . 2017 May; 60(12):5193-5208. PMID: 28541707
PI3Kδ plays an important role controlling immune cell function and has therefore been identified as a potential target for the treatment of immunological disorders. This article highlights our work toward...
4.
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors
Qin L, Ruan Z, Cherney R, Murali Dhar T, Neels J, Weigelt C, et al.
Bioorg Med Chem Lett . 2017 Jan; 27(4):855-861. PMID: 28108251
As demonstrated in preclinical animal models, the disruption of PI3Kδ expression or its activity leads to a decrease in inflammatory and immune responses. Therefore, inhibition of PI3Kδ may provide an...
5.
Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors
Bhide R, Neels J, Qin L, Ruan Z, Stachura S, Weigelt C, et al.
Bioorg Med Chem Lett . 2016 Aug; 26(17):4256-60. PMID: 27476421
Aberrant Class I PI3K signaling is a key factor contributing to many immunological disorders and cancers. We have identified 4-amino pyrrolotriazine as a novel chemotype that selectively inhibits PI3Kδ signaling...
6.
Design, synthesis, functional and structural characterization of an inhibitor of N-acetylneuraminate-9-phosphate phosphatase: observation of extensive dynamics in an enzyme/inhibitor complex
Kim S, Constantine K, Duke G, Goldfarb V, Hunt J, Johnson S, et al.
Bioorg Med Chem Lett . 2013 Jun; 23(14):4107-11. PMID: 23747226
The design, synthesis and characterization of a phosphonate inhibitor of N-acetylneuraminate-9-phosphate phosphatase (HDHD4) is described. Compound 3, where the substrate C-9 oxygen was replaced with a nonlabile CH2 group, inhibits...
7.
The antiangiogenic activity in xenograft models of brivanib, a dual inhibitor of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinases
Bhide R, Lombardo L, Hunt J, Cai Z, Barrish J, Galbraith S, et al.
Mol Cancer Ther . 2010 Jan; 9(2):369-78. PMID: 20103604
Tumor angiogenesis is a complex and tightly regulated network mediated by various proangiogenic factors. The fibroblast growth factor (FGF) and vascular endothelial growth factor (VEGF) family of growth factors, and...
8.
Metabolism of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737): identification of an unusual N-acetylglucosamine conjugate in the cynomolgus monkey
Johnson B, Kamath A, Leet J, Liu X, Bhide R, Tejwani R, et al.
Drug Metab Dispos . 2008 Sep; 36(12):2475-83. PMID: 18787055
5-Isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737) is a potent and selective vascular endothelial growth factor receptor-2 antagonist. In this study, liquid chromatography/tandem mass spectrometry and NMR were used to investigate the biotransformation of BMS-645737...
9.
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor
Ruel R, Thibeault C, LHeureux A, Martel A, Cai Z, Wei D, et al.
Bioorg Med Chem Lett . 2008 Apr; 18(9):2985-9. PMID: 18395443
We report herein a series of substituted N-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amines as inhibitors of vascular endothelial growth factor receptor-2 tyrosine kinase. Through structure-activity relationship studies, biochemical potency, pharmacokinetics, and kinase selectivity were optimized...
10.
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 novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast...
Cai Z, Zhang Y, Borzilleri R, Qian L, Barbosa S, Wei D, et al.
J Med Chem . 2008 Feb; 51(6):1976-80. PMID: 18288793
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 of the...