Isoform-selective PI3K inhibitors for various diseases

RRY Bheemanaboina - Current topics in medicinal chemistry, 2020 - ingentaconnect.com
Phosphoinositide 3-kinases (PI3Ks) are a family of ubiquitously distributed lipid kinases that
control a wide variety of intracellular signaling pathways. Over the years, PI3K has emerged …

Thiazolidone derivatives as inhibitors of chikungunya virus

SS Jadav, BN Sinha, R Hilgenfeld, B Pastorino… - European Journal of …, 2015 - Elsevier
A series of arylalkylidene derivatives of 1, 3-thiazolidin-4-one (1–20) were synthesized and
tested for their antiviral activity against chikungunya virus (LR2006_OPY1) in Vero cell …

5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl)alkancarboxylic Acids as Antimicrobial Agents: Synthesis, Biological Evaluation, and Molecular Docking …

V Horishny, V Kartsev, A Geronikaki, V Matiychuk… - Molecules, 2020 - mdpi.com
Background: Infectious diseases symbolize a global consequential strain on public health
security and impact on the socio-economic stability all over the world. The increasing …

Synthesis of 5-arylidenerhodanines in L-proline-based deep eutectic solvent

S Hesse - Beilstein Journal of Organic Chemistry, 2023 - beilstein-journals.org
Rhodanines and their derivatives are known to have many pharmacological activities that
can be modulated through different functionalization sites. One of the most studied …

Leucettamine B analogs and their carborane derivative as potential anti-cancer agents: Design, synthesis, and biological evaluation

MH Hsu, CY Hsieh, M Kapoor, JH Chang, HL Chu… - Bioorganic …, 2020 - Elsevier
Leucettamine B is a natural product found in marine sponge Leucetta microraphis. Several
of analogs of its family, such as aplysinopsine and clathridine, are medicinally active …

Exploration of a series of 5-arylidene-2-thioxoimidazolidin-4-ones as inhibitors of the cytolytic protein perforin

JA Spicer, G Lena, DM Lyons… - Journal of medicinal …, 2013 - ACS Publications
A series of novel 5-arylidene-2-thioxoimidazolidin-4-ones were investigated as inhibitors of
the lymphocyte-expressed pore-forming protein perforin. Structure–activity relationships …

Biological evaluation and docking studies of recently identified inhibitors of phosphoinositide-3-kinases

DA Sabbah, NA Simms, MG Brattain… - Bioorganic & medicinal …, 2012 - Elsevier
The alpha isoform of the phosphatidylinositol-3-kinases (PI3Kα) is often mutated, amplified
and overexpressed in human tumors. In an effort to develop new inhibitors targeting this …

A novel PI3K inhibitor PIK-C98 displays potent preclinical activity against multiple myeloma

J Zhu, M Wang, Y Yu, H Qi, K Han, J Tang… - …, 2014 - pmc.ncbi.nlm.nih.gov
Recent clinical trials have demonstrated targeting PI3K pathway is a promising strategy for
the treatment of blood cancers. To identify novel PI3K inhibitors, we performed a high …

Evaluation of Michael-type Acceptor Reactivity of 5-Benzylidenebarbiturates, 5-benzylidenerhodanines, and Related Heterocycles Using NMR.

E Arsovska, J Trontelj, N Zidar… - Acta Chimica …, 2014 - search.ebscohost.com
Despite existing experimental and computational tools to assess the risk, the non-specific
chemical modification of protein thiol groups remains a significant source of false-positive …

Synthesis and pharmacological evaluation of 4-iminothiazolidinones for inhibition of PI3 kinase

JA Pinson, O Schmidt-Kittler, M Frazzetto… - Australian journal of …, 2012 - CSIRO Publishing
The thiazolidinedione, compound 1, has previously shown pan-inhibition of the
phosphoinositide 3-kinase (PI3K) class I isoforms. We hypothesized the derivatization of the …