26488-79-9Relevant academic research and scientific papers
Molecular probe derived from calcium-sensitive receptor protein antagonist and application of molecular probe in parathyroid gland resection surgery
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Paragraph 0048; 0072-0073; 0075, (2021/07/28)
The invention discloses a molecular probe derived from a calcium-sensitive receptor protein antagonist and application of the molecular probe in parathyroid gland resection surgery. The molecular probe is specifically a molecular probe which is derived fr
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models
Nguyen, William,Jacobson, Jonathan,Jarman, Kate E.,Jousset Sabroux, Helene,Harty, Leigh,McMahon, James,Lewin, Sharon R.,Purcell, Damian F.,Sleebs, Brad E.
, p. 5148 - 5175 (2019/05/28)
The persistent reservoir of cells latently infected with human immunodeficiency virus (HIV)-integrated proviral DNA necessitates lifelong suppressive antiretroviral therapy (ART). Epigenetic targeted compounds have shown promise as potential latency-reversing agents; however, these drugs have undesirable toxicity and lack specificity for HIV. We utilized a novel HEK293-derived FlpIn dual-reporter cell line, which quantifies specific HIV provirus reactivation (LTR promoter) relative to nonspecific host cell gene expression (CMV promoter), to identify the 5-substituted 2-acylaminothiazole hit class. Here, we describe the optimization of the hit class, defining the functionality necessary for HIV gene activation and for improving in vitro metabolism and solubility. The optimized compounds displayed enhanced HIV gene expression in HEK293 and Jurkat 10.6 latency cellular models and increased unspliced HIV RNA in resting CD4+ T cells isolated from HIV-infected individuals on ART, demonstrating the potential of the 2-acylaminothiazole class as latency-reversing agents.
Design, synthesis and preliminary bioactivity evaluations of 8-hydroxyquinoline derivatives as matrix metalloproteinase (MMP) inhibitors
Chen, Chen,Yang, Xinying,Fang, Hao,Hou
, (2019/08/13)
Matrix metalloproteinases (MMPs) play important roles in many diseases including cancer. With moderate metal-binding affinity, 8-hydroxyquinoline has gained much interest in current drug design and development. Specially, it has been reported that 8-hydroxyquinoline derivatives serve as MMP-2 inhibitors with micromolar IC50 values. In the current study, a series of 8-hydroxyquinoline derivatives were designed and synthesized as new MMP-2 and MMP-9 inhibitors. The most active compounds 5e and 5h not only displayed good inhibitory activities against MMP-2/9 with IC50 at submicromolar level, but also possessed potent anti-proliferative, anti-invasive and anti-angiogenesis activity in A549 cell line. Western blot also revealed that 5e and 5h down-regulate the expression of MMP-2 and MMP-9 in A549 cell line. Moreover, flow cytometry analysis indicated that compound 5e could promote apoptosis of A549 cells in vitro. Molecular docking analysis also revealed favorable binding modes of 5e in the active sites of MMP-2 and MMP-9.
ACTIVATORS OF HIV LATENCY
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Page/Page column 41; 58; 59, (2018/04/19)
The present invention relates to novel compounds which active HIV expression in latently infected cells. More particularly, the invention relates to pharmaceutical compositions comprising the novel compounds and their use in activating HIV expression in latently infected cells. Further still, the invention relates to pharmaceutical compositions comprising the novel compounds in combination with anti-HIV therapy compounds and their use in treating HIV infection in both animals and humans. The invention further provides means for preparing the compounds.
Ultrasound stimulated nucleation and growth of a dye assembly into extended gel nanostructures
Malicka, Joanna M.,Sandeep, Anjamkudy,Monti, Filippo,Bandini, Elisa,Gazzano, Massimo,Ranjith, Choorikkat,Praveen, Vakayil K.,Ajayaghosh, Ayyappanpillai,Armaroli, Nicola
supporting information, p. 12991 - 13001 (2013/10/01)
A squaraine dye functionalized with a bulky trialkoxy phenyl moiety through a flexible diamide linkage (GA-SQ) capable of undergoing self-assembly has been synthesized and fully characterized. Rapid cooling of a hot solution of GA-SQ to 0 °C results in se
Pyrimidine derivatives
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, (2008/06/13)
The present invention relates to novel 5-(ω-substituted amino-alkanoyl amino)pyrimidine derivatives, processes for producing the derivatives, and pharmaceutical compositions containing said derivatives. The compounds in the present invention have potent effects of inhibiting ACAT activity and lowering serum cholesterol. The compounds of the present invention are extremely useful for the treatment and/or prevention of arteriosclerosis or hyperlipidemia.
Aggregation of a Surfactant Squaraine in Langmuir-Blodgett Films, Solids, and Solution
Chen, Huijuan,Herkstroeter, William G.,Perlstein, Jerome,Law, Kock-Yee,Whitten, David G
, p. 5138 - 5146 (2007/10/02)
The aggregation of a surfactant squaraine, 4-(N-methyl-N-(carboxypropyl)amino)phenyl-4'-(N,N-dibutylamino)phenylsquaraine (SBA), has been studied in a variety of media, including organic solvents, aqueous cyclodextrin (CD) solutions, vesicles, monolayers,
