Vinod F Patel
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Explore the profile of Vinod F Patel including associated specialties, affiliations and a list of published articles.
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34
Citations
339
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Recent Articles
1.
Barberis C, Erdman P, Czekaj M, Fire L, Pribish J, Tserlin E, et al.
Bioorg Med Chem Lett
. 2020 Oct;
30(23):127625.
PMID: 33096160
N-substituted azaindoles were discovered as potent pan-PIM inhibitors. Lead optimization, guided by structure and focused on physico-chemical properties allowed us to solve inherent hERG and permeability liabilities, and provided compound...
2.
Geuns-Meyer S, Cee V, Deak H, Du B, Hodous B, Nguyen H, et al.
J Med Chem
. 2015 May;
58(13):5189-207.
PMID: 25970324
Efforts to improve upon the physical properties and metabolic stability of Aurora kinase inhibitor 14a revealed that potency against multidrug-resistant cell lines was compromised by increased polarity. Despite its high...
3.
Cheng Y, Brown J, Judd T, Lopez P, Qian W, Powers T, et al.
ACS Med Chem Lett
. 2015 Feb;
6(2):210-5.
PMID: 25699151
BACE1 inhibition to prevent Aβ peptide formation is considered to be a potential route to a disease-modifying treatment for Alzheimer's disease. Previous efforts in our laboratory using a combined structure-...
4.
Chen J, Liu Q, Yuan C, Gore V, Lopez P, Ma V, et al.
Bioorg Med Chem Lett
. 2015 Jan;
25(4):767-74.
PMID: 25613679
The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer's disease. We used a structure- and property-based...
5.
Epstein O, Bryan M, Cheng A, Derakhchan K, Dineen T, Hickman D, et al.
J Med Chem
. 2014 Nov;
57(23):9796-810.
PMID: 25389560
The optimization of a series of aminooxazoline xanthene inhibitors of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) is described. An early lead compound showed robust Aβ lowering activity in...
6.
Dineen T, Chen K, Cheng A, Derakhchan K, Epstein O, Esmay J, et al.
J Med Chem
. 2014 Nov;
57(23):9811-31.
PMID: 25363711
We have previously shown that the aminooxazoline xanthene scaffold can generate potent and orally efficacious BACE1 inhibitors although certain of these compounds exhibited potential hERG liabilities. In this article, we...
7.
Huang H, Acquaviva L, Berry V, Bregman H, Chakka N, OConnor A, et al.
ACS Med Chem Lett
. 2014 Jun;
3(12):1059-64.
PMID: 24900428
Aberrant activation of the Wnt pathway is believed to drive the development and growth of some cancers. The central role of CK1γ in Wnt signal transduction makes it an attractive...
8.
Pennington L, Whittington D, Bartberger M, Jordan S, Monenschein H, Nguyen T, et al.
Bioorg Med Chem Lett
. 2013 Jun;
23(15):4459-64.
PMID: 23769639
We describe a systematic study of how macrocyclization in the P₁-P₃ region of hydroxyethylamine-based inhibitors of β-site amyloid precursor protein (APP)-cleaving enzyme (BACE1) modulates in vitro activity. This study reveals...
9.
Huang H, La D, Cheng A, Whittington D, Patel V, Chen K, et al.
J Med Chem
. 2012 Aug;
55(21):9156-69.
PMID: 22928914
A structure- and property-based drug design approach was employed to identify aminooxazoline xanthenes as potent and selective human β-secretase inhibitors. These compounds exhibited good isolated enzyme, cell potency, and selectivity...
10.
Hua Z, Huang X, Bregman H, Chakka N, DiMauro E, Doherty E, et al.
Bioorg Med Chem Lett
. 2012 Aug;
22(17):5392-5.
PMID: 22877629
Screening of the Amgen compound library led to the identification of 2-phenylamino-6-cyano-1H-benzimidazole 1a as a potent CK1 gamma inhibitor with excellent kinase selectivity and unprecedented CK1 isoform selectivity. Further structure-based...