ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTChemical relaxation and equilibrium studies of association in aqueous solutions of bolaform detergents. 1. Dodecane-1,12-bis(trimethylammonium bromide)S. Yiv, K. M. Kale, J. Lang, and R. ZanaCite this: J. Phys. Chem. 1976, 80, 24, 2651–2655Publication Date (Print):November 1, 1976Publication History Published online1 May 2002Published inissue 1 November 1976https://pubs.acs.org/doi/10.1021/j100565a006https://doi.org/10.1021/j100565a006research-articleACS PublicationsRequest reuse permissionsArticle Views160Altmetric-Citations50LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access options Get e-Alerts
Introduction: A focal point in contemporary research aimed at preventing the heterosexual spread of AIDS has been the development of intravaginal anti-HIV microbicides to curb the mucosal human immunodeficiency virus type 1 (HIV-1) transmission. Areas covered: This article reviews the preclinical activity and safety profile of the thiophene thiourea PETT derivative, HI-443 (N′-[2-(2-thiophene)ethyl]-N′-[2-(5-bromopyridyl)] thiourea]). HI-443 is a rationally designed non-nucleoside reverse transcriptase inhibitor (NNRTI) with unprecedented activity against primary clinical HIV-1 isolates with NRTI or NNRTI resistance, multidrug resistance as well as non-B envelope subtypes of HIV-1. HI-443 exhibited a favorable toxicity and pharmacokinetics profile following oral, intraperitoneal or intravenous administration in rodents and a favorable safety profile after repeated intravaginal dosing via a gel formulation in rabbits and pigs. HI-443 did not induce the secretion of pro-inflammatory cytokines and chemokines by three-dimensional reconstituted human vaginal epithelia integrating Langerhans cells ex vivo or in the in vivo porcine model at therapeutic dose levels. Intravaginally administered HI-443 prevented vaginal transmission of a drug-resistant clinical HIV-1 isolate in the surrogate Hu-PBL-SCID mouse model of AIDS. Expert opinion: The discovery of HI-443 as a non-spermicidal broad-spectrum antiretroviral agent represents a significant step forward in the development of a prophylactic microbicide without contraceptive activity for curbing heterosexual HIV transmission.
The quinazoline derivative 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P131/JANEX-1; CAS 202475-60-3) is a dual-function inhibitor of Janus kinase 3 (JAK3) and Epidermal Growth Factor (EGF) receptor kinase.A PEGylated liposomal nanoparticle formulation of GMP-grade WHI-P131 exhibited potent in vivo activity against breast cancer cells.Notably, this therapeutic nanoparticle formulation of GMP-grade WHI-P131 was substantially more effective than the standard chemotherapy drugs paclitaxel, gemcitabine, and gefi tinib against chemotherapy-resistant breast cancer in the MMTV/Neu transgenic mouse model.These experimental results demonstrate that the nanotechnologyenabled delivery of WHI-P131 shows therapeutic potential against breast cancer.
