Tarek S Mansour
Overview
Explore the profile of Tarek S Mansour including associated specialties, affiliations and a list of published articles.
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Articles
72
Citations
1131
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Recent Articles
1.
Mansour T, Pallepati R, Basetti V
Bioorg Med Chem Lett
. 2020 Jul;
30(16):127288.
PMID: 32631510
Modifications at C and C positions of 3-cyanoquinolines 6 and 7 led to potent inhibitors of the ErbB family of kinases particularly against EGFR and Her4 enzymes in the radioisotope...
2.
Halaban R, Bacchiocchi A, Straub R, Cao J, Sznol M, Narayan D, et al.
Oncotarget
. 2019 May;
10(23):2237-2251.
PMID: 31040916
The major drawback of melanoma therapy with BRAF and MAPK inhibitors is the innate and acquired drug resistance. We therefore explored alternative targets and developed a new compound, SAB298, that...
3.
Mansour T, Potluri V, Pallepati R, Basetti V, Keesara M, Moghudula A, et al.
Bioorg Med Chem Lett
. 2019 Apr;
29(12):1435-1439.
PMID: 31023512
No abstract available.
4.
Focken T, Liu S, Chahal N, Dauphinais M, Grimwood M, Chowdhury S, et al.
ACS Med Chem Lett
. 2016 Mar;
7(3):277-82.
PMID: 26985315
We report on a novel series of aryl sulfonamides that act as nanomolar potent, isoform-selective inhibitors of the human sodium channel hNaV1.7. The optimization of these inhibitors is described. We...
5.
Wan Z, Chenail E, Li H, Ipek M, Xiang J, Suri V, et al.
ACS Med Chem Lett
. 2014 Jun;
4(1):118-23.
PMID: 24900572
11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the conversion of inactive glucocorticoid cortisone to its active form, cortisol. The glucocorticoid receptor (GR) signaling pathway has been linked to the pathophysiology of...
6.
Kaila N, Follows B, Leung L, Thomason J, Huang A, Moretto A, et al.
J Med Chem
. 2014 Feb;
57(4):1299-322.
PMID: 24512187
Previously we reported the discovery of CRA-898 (1), a diazine indole acetic acid containing CRTH2 antagonist. This compound had good in vitro and in vivo potency, low rates of metabolism,...
7.
Kaila N, Huang A, Moretto A, Follows B, Janz K, Lowe M, et al.
J Med Chem
. 2012 Jun;
55(11):5088-109.
PMID: 22651823
New classes of CRTH2 antagonists, the pyridazine linker containing indole acetic acids, are described. The initial hit 1 had good potency but poor permeability, metabolic stability, and PK. Initial optimization...
8.
Wu Y, Li J, Wu J, Morgan P, Xu X, Rancati F, et al.
Bioorg Med Chem Lett
. 2011 Dec;
22(1):138-43.
PMID: 22153340
Chronic obstructive pulmonary disease (COPD) is an inflammatory lung disease associated with irreversible progressive airflow limitation. Matrix metalloproteinase-12 (MMP-12) has been characterized to be one of the major proteolytic enzymes...
9.
Synthesis of potent and orally efficacious 11β-hydroxysteroid dehydrogenase type 1 inhibitor HSD-016
Wan Z, Chenail E, Li H, Kendall C, Wang Y, Gingras S, et al.
J Org Chem
. 2011 Jul;
76(17):7048-55.
PMID: 21736359
Cortisol and the glucocorticoid receptor (GR) signaling pathway has been linked to the development of diabetes and metabolic syndrome. In vivo, 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the conversion of...
10.
Venkatesan A, Chen Z, dos Santos O, Dehnhardt C, Santos E, Ayral-Kaloustian S, et al.
Bioorg Med Chem Lett
. 2010 Aug;
20(19):5869-73.
PMID: 20797855
A series of mono-morpholino 1,3,5-triazine derivatives (8a-8q) bearing a 3-oxa-8-azabicyclo[3.2.1]octane were prepared and evaluated for PI3-kinase/mTOR activity. Replacement of one of the bis-morpholines in lead compound 1 (PKI-587) with 3-oxa-8-azabicyclo[3.2.1]octane...