Edgars Jecs
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Explore the profile of Edgars Jecs including associated specialties, affiliations and a list of published articles.
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11
Citations
54
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Recent Articles
1.
Jecs E, Tahirovic Y, Wilson R, Miller E, Kim M, Truax V, et al.
J Med Chem
. 2022 Feb;
65(5):4058-4084.
PMID: 35179893
Our first-generation CXCR4 antagonist TIQ15 was rationally modified to improve drug-like properties. Introducing a nitrogen atom into the aromatic portion of the tetrahydroisoquinoline ring led to several heterocyclic variants including...
2.
Nguyen H, Tahirovic Y, Truax V, Wilson R, Jecs E, Miller E, et al.
ACS Med Chem Lett
. 2021 Oct;
12(10):1605-1612.
PMID: 34676043
This work surveys a variety of diamino-heterocycles as an isosteric replacement for the piperazine substructure of our previously disclosed piperarinyl-tetrahydroisoquinoline containing CXCR4 antagonists. A late-stage Buchwald coupling route was developed...
3.
Pribut N, Kaiser T, Wilson R, Jecs E, Dentmon Z, Pelly S, et al.
ACS Infect Dis
. 2020 Apr;
6(5):922-929.
PMID: 32275393
A series of five benzimidazole-based compounds were identified using a machine learning algorithm as potential inhibitors of the respiratory syncytial virus (RSV) fusion protein. These compounds were synthesized, and compound...
4.
Tahirovic Y, Pelly S, Jecs E, Miller E, Sharma S, Liotta D, et al.
Expert Opin Ther Pat
. 2019 Dec;
30(2):87-101.
PMID: 31854208
: The chemokine receptor CXCR4 has been under intense study due to the central role it plays in immune system regulation and the pathology of many human diseases. The FDA...
5.
Nguyen H, Kim M, Wilson R, Butch C, Kuo K, Miller E, et al.
J Med Chem
. 2018 Jul;
61(16):7168-7188.
PMID: 30052039
CXCR4 is a G-protein-coupled receptor that interacts with its cognate ligand, CXCL12, to synchronize many physiological responses and pathological processes. Disruption of the CXCL12-CXCR4 circuitry by small-molecule antagonists has emerged...
6.
Discovery of -Alkyl Piperazine Side Chain Based CXCR4 Antagonists with Improved Drug-like Properties
Tahirovic Y, Truax V, Wilson R, Jecs E, Nguyen H, Miller E, et al.
ACS Med Chem Lett
. 2018 May;
9(5):446-451.
PMID: 29795757
A novel series of CXCR4 antagonists with piperidinyl and piperazinyl alkylamine side chains designed as butyl amine replacements are described. Several of these compounds showed similar activity to the parent...
7.
Jecs E, Miller E, Wilson R, Nguyen H, Tahirovic Y, Katzman B, et al.
ACS Med Chem Lett
. 2018 Feb;
9(2):89-93.
PMID: 29456793
A structure-activity relationship study of potent TIQ15-derived CXCR4 antagonists is reported. In this investigation, the TIQ15 side-chain was constrained to improve its drug properties. The cyclohexylamino congener was found to...
8.
Miller E, Jecs E, Truax V, Katzman B, Tahirovic Y, Wilson R, et al.
J Med Chem
. 2018 Jan;
61(3):946-979.
PMID: 29350534
CXCR4 is a seven-transmembrane receptor expressed by hematopoietic stem cells and progeny, as well as by ≥48 different cancers types. CXCL12, the only chemokine ligand of CXCR4, is secreted within...
9.
Wilson R, Jecs E, Miller E, Nguyen H, Tahirovic Y, Truax V, et al.
ACS Med Chem Lett
. 2018 Jan;
9(1):17-22.
PMID: 29348805
CXCR4 is the most common chemokine receptor expressed on the surface of many cancer cell types. In comparison to normal cells, cancer cells overexpress CXCR4, which correlates with cancer cell...
10.
Jecs E, Diver S
Org Lett
. 2015 Jun;
17(14):3510-3.
PMID: 26114894
The total synthesis of amphidinolide P was achieved through two different ene-yne metathesis approaches. In each approach, the metathesis step was performed at late stages in the synthesis with all...