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Owen B Wallace

Explore the profile of Owen B Wallace including associated specialties, affiliations and a list of published articles. Areas
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Articles 14
Citations 165
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Recent Articles
1.
Wang T, Wallace O, Zhang Z, Fang H, Yang Z, Robinson B, et al.
Bioorg Med Chem Lett . 2019 Apr; 29(11):1423-1429. PMID: 30940396
Indole- and azaindole-based glyoxylyl amide derivatives have been described as HIV-1 attachment inhibitors (AIs) that act by blocking the interaction between the viral gp120 coat protein and the human host...
2.
Meanwell N, Wallace O, Wang H, Deshpande M, Pearce B, Trehan A, et al.
Bioorg Med Chem Lett . 2009 Jul; 19(17):5136-9. PMID: 19632112
1-(4-Benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione (1a) has been characterized as an inhibitor of HIV-1 attachment that interferes with the interaction of viral gp120 with the host cell receptor CD4. In previous studies, the effect...
3.
Meanwell N, Wallace O, Fang H, Wang H, Deshpande M, Wang T, et al.
Bioorg Med Chem Lett . 2009 Mar; 19(7):1977-81. PMID: 19251416
The effects of introducing simple halogen, alkyl, and alkoxy substituents to the 4, 5, 6 and 7 positions of 1-(4-benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione, an inhibitor of the interaction between HIV gp120 and host...
4.
Parker M, Barten D, Bergstrom C, Bronson J, Corsa J, Deshpande M, et al.
Bioorg Med Chem Lett . 2007 Jul; 17(16):4432-6. PMID: 17606371
A series of N-alkylbenzenesulfonamides were developed from a high throughput screening hit. Classic and parallel synthesis strategies were employed to produce compounds with good in vitro and in vivo gamma-secretase...
5.
Richardson T, Frank S, Wang M, Clarke C, Jones S, Ying B, et al.
Bioorg Med Chem Lett . 2007 May; 17(13):3544-9. PMID: 17482463
Structure-activity relationship studies are described, which led to the discovery of novel selective estrogen receptor modulators (SERMs) for the potential treatment of uterine fibroids. The SAR studies focused on limiting...
6.
Wallace O, Lauwers K, Dodge J, May S, Calvin J, Hinklin R, et al.
J Med Chem . 2006 Feb; 49(3):843-6. PMID: 16451049
A selective estrogen receptor modulator (SERM) for the potential treatment of hot flushes is described. (R)-(+)-7,9-difluoro-5-[4-(2-piperidin-1-ylethoxy)phenyl]-5H-6-oxachrysen-2-ol, LSN2120310, potently binds ERalpha and ERbeta and is an antagonist in MCF-7 breast adenocarcinoma...
7.
Hummel C, Geiser A, Bryant H, Cohen I, Dally R, Fong K, et al.
J Med Chem . 2005 Oct; 48(22):6772-5. PMID: 16250633
The design of a novel selective estrogen receptor modulator (SERM) for the potential treatment of uterine leiomyoma is described. 16 (LY2066948-HCl) binds with high affinity to estrogen receptors alpha and...
8.
Geiser A, Hummel C, Draper M, Henck J, Cohen I, Rudmann D, et al.
Endocrinology . 2005 Jul; 146(10):4524-35. PMID: 16002528
The use of selective estrogen receptor modulators for the treatment of estrogen-dependent diseases in premenopausal women has been hindered by undesirable ovarian stimulation and associated risks of ovarian cysts. We...
9.
Wallace O, Bryant H, Shetler P, Adrian M, Geiser A
Bioorg Med Chem Lett . 2004 Sep; 14(20):5103-6. PMID: 15380208
For selective estrogen receptor modulators (SERMs), the orientation of the basic side chain relative to the SERM core has a significant impact on function. The synthesis and biological evaluation of...
10.
Prasad C, Wallace O, Noonan J, Sloan C, Lau W, Vig S, et al.
Bioorg Med Chem Lett . 2004 Mar; 14(8):1917-21. PMID: 15050627
Using a cell-based assay, we have identified optimal residues and key recognition elements necessary for inhibition of gamma-secretase. An (S)-hydroxy group or 3,5-difluorophenylacetyl group at the amino terminus and N-methyltertiary...