Výsledky vyhledávání - "Douglas Erbeck"

Anti-cancer Activity Profile of 3’-Azidothymidine 5’- [p-Methoxyphenyl Methoxyalaninyl Phosphate] (Compound 003), a Novel Nucleoside Analog

Autor: Taracad K. Venkatachalam, Douglas Erbeck, Fatih M. Uckun, Xing-Ping Liu, Sanjive Qazi, Ilker Dibirdik, Heather E. Tibbles, Alexei O. Vassilev

Publikováno v: Arzneimittelforschung. 54:715-731

The novel cytotoxic nucleoside analog Compound 003 (3'-azidothymidine 5'-[p-methoxyphenyl methoxyalaninyl phosphate], CAS 149560-32-7) prevented bipolar mitotic spindle assembly and caused a G2 arrest in human cancer cells. Compound 003 was very well

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::876803f4c3f1264b8981dfbf91aadd95
https://doi.org/10.1055/s-0031-1297029

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Effect of Targeting Janus Kinase 3 on the Development of Intestinal Tumors in the Adenomatous Polyposis Colimin Mouse Model of Familial Adenomatous Polyposis

Autor: Fatih M. Uckun, Alexei O. Vassilev, Douglas Erbeck, Sanjive Qazi, Taracad K. Venkatachalam, Heather E. Tibbles

Publikováno v: Arzneimittelforschung. 57:320-329

Familial adenomatous polyposis (FAP) is associated with germ-line mutations in the tumor suppressor gene, adenomatous polyposis coli (APC) located on chromosome 5q21. Multiple intestinal neoplasia (Min) in mice resembles FAP in humans, resulting from

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34420cd853484dc5de82ab3d28a0f545
https://doi.org/10.1055/s-0031-1296626

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In vivo Pharmacokinetics, Metabolism, Toxicity, and Anti-HIV Activity of N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]thiourea (HI-443), a Potent Non-nucleoside Inhibitor of HIV Reverse Transcriptase

Autor: Douglas Erbeck, Taracad K. Venkatachalam, Fatih M. Uckun, Heather E. Tibbles

Publikováno v: Arzneimittelforschung. 57:483-496

N'-[2-(2-Thiophene)ethyl]-N'-[2-(5bromopyridyl)]thiourea (CAS 258340-15-7, HI-443) is a potent non-nucleoside inhibitor of HIV reverse transcriptase (NNRTI) that was rationally designed as a candidate anti-HIV agent. The purpose of the present study

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::901d205ca8d9b96a0cdc2dbdf847e17e
https://doi.org/10.1055/s-0031-1296636

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Developmental Toxicology Studies of WHI-07, a Novel Nucleoside Analogue-Based Dual-Function Microbicide, Administered Intravaginally to Rabbits

Autor: Douglas Erbeck, Osmond J. D'Cruz, Fatih M. Uckun

Publikováno v: Toxicologic Pathology. 31:698-708

The zidovudine derivative, 5-bromo-6-methoxy-5,6-dihydro-3-azidothymidine-5'-( p-bromophenyl) methoxy alaninyl phosphate (WHI-07), is a dual-function spermicidal and anti-HIV agent with contraceptive and microbicidal activity. In previous subchronic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8bd96e2e875ea7d0dc6d2328423abbcb
https://doi.org/10.1080/01926230390241936

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Two-year toxicity and carcinogenicity studies in B6C3F1 mice with 5-bromo-6-methoxy-5,6-dihydro-3′-azidothymidine-5′-(p-bromophenyl) methoxyalaninyl phosphate (WHI-07), a novel anti-HIV and contraceptive agent

Autor: Douglas Erbeck, Osmond J. D'Cruz, Barbara Waurzyniak, Fatih M. Uckun

Publikováno v: Toxicology. 179:61-77

The zidovudine derivative, 5-bromo-6-methoxy-5,6-dihydro-3'-azidothymidine-5'-(p-bromophenyl) methoxy alaninyl phosphate (WHI-07), is a dual-function spermicidal and anti-HIV agent with contraceptive and microbicidal activity. In previous two subchro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b072df08a634b798d3aea52e9f626907
https://doi.org/10.1016/s0300-483x(02)00319-0

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In vivo pharmacokinetics and toxicity of a novel hydrophilic oral formulation of the potent non-nucleoside reverse transcriptase inhibitor compound N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443)

Autor: Heather E. Tibbles, Sanjive Qazi, Douglas Erbeck, Fatih M. Uckun, Taracad K. Venkatachalam

Publikováno v: Arzneimittel-Forschung. 57(4)

The thiophene ethyl thiourea (TET) compound N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443) is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI). The pharmacokinetics of 17 different novel oral formulations of HI-443

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e078c7d3396dbe0f788ebb7520107dfd
https://pubmed.ncbi.nlm.nih.gov/17515292

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Improved oral bioavailability of anti-HIV agent N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443) in a novel lipophilic formulation

Autor: Heather E. Tibbles, Taracad K. Venkatachalam, Sanjive Qazi, Douglas Erbeck, Fatih M. Uckun

Publikováno v: Arzneimittel-Forschung. 57(3)

N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (CAS 258340-15-7, HI-443) is a rationally designed non-nucleoside reverse transcriptase inhibitor (NNRTI) with potent anti-HIV activity at nanomolar concentrations but poor oral bioavailabili

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8789cbc90ae641d4d577e5cb01b2c8e
https://pubmed.ncbi.nlm.nih.gov/17469651

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Preclinical toxicity and pharmacokinetics of the Bruton's tyrosine kinase-targeting anti-leukemic drug candidate, alpha-cyano-beta-hydroxy-beta-methyl-N- (2,5-dibromophenyl) propenamide (LFM-A13)

Autor: Darin DuMez, Fatih M. Uckun, Heather Tibbies, Douglas Erbeck, Taracad K. Venkatachalam

Publikováno v: Arzneimittel-Forschung. 57(1)

The leflunomide (CAS 75706-12-6) metabolite (LFM) analog alpha-cyano-beta-hydroxy-beta-methyl-N-(2,5-dibromophenyl)-propenamide (LFM-A13, DDE-28, CAS 244240-24-2) is a rationally-designed specific inhibitor of the TEC family protein tyrosine kinase,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60ba89e314571e5bce6f2f3fe5921891
https://pubmed.ncbi.nlm.nih.gov/17341007

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Developmental safety profile of the anti-HIV agent stampidine in rabbits

Autor: Fatih M. Uckun, Douglas Erbeck, Osmond J. D'Cruz

Publikováno v: Arzneimittel-Forschung. 56(2A)

Stampidine (STAMP, DDE-113, HI-113, N-[p-(4-bromophenyl)-2',3'-didehydro-3'-deoxy-5'-thymidylyl]-L-alanine methyl ester, CAS 217178-62-6) is a novel aryl phosphate derivative of stavudine (STV, d4T, 2',3'-didehydro-3'-deoxythymidine, CAS 3056-17-5) w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db84427e31eb2427d9e3d75ff362fd13
https://pubmed.ncbi.nlm.nih.gov/16570824

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