Synthesis and biological evaluation of new 2-(6-alkyl-pyrazin-2-yl)-1H-benz[d]imidazoles as potent anti-inflammatory and antioxidant agents
Sign Up to like & getrecommendations! Published in 2017 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-017-1897-7
Abstract: A novel series of 2-(6-alkyl-pyrazin-2-yl)-1H-benzo[d]imidazole analogs (3a–3j) derived from 2-(6-chloropyrazin-2-yl)-1H-benzo[d]imidazole (2) by reacting with various substituted cyclic and acyclic secondary amines in presence of Pd-PEPPSI Mes catalyst by using Buchwald–Hartwig amination in excellent yield. The… read more here.
Keywords: anti inflammatory; potent anti; alkyl pyrazin; inflammatory ... See more keywords
Exploring the cycloheptathiophene-3-carboxamide scaffold to disrupt the interactions of the influenza polymerase subunits and obtain potent anti-influenza activity.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.06.015
Abstract: With the aim to identify small molecules able to disrupt PA-PB1 subunits interaction of influenza virus (flu) RNA-dependent RNA polymerase, and based on previous structural and computational information, in this paper we have designed and… read more here.
Keywords: carboxamide scaffold; potent anti; exploring cycloheptathiophene; scaffold disrupt ... See more keywords
Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D
Sign Up to like & getrecommendations! Published in 2019 at "European Journal of Medicinal Chemistry"
DOI: 10.1016/j.ejmech.2018.11.068
Abstract: Following up the open initiative of anti-malarial drug discovery, a GlaxoSmithKline (GSK) phenotypic screening hit was developed to generate hydroxyethylamine based plasmepsin (Plm) inhibitors exhibiting growth inhibition of the malaria parasite Plasmodium falciparum at nanomolar… read more here.
Keywords: potent anti; malarial activity; anti malarial; plasmepsin ... See more keywords
Identification of tetragocarbone C and sideroxylin as the most potent anti-inflammatory components of Syncarpia glomulifera.
Sign Up to like & getrecommendations! Published in 2021 at "Fitoterapia"
DOI: 10.1016/j.fitote.2021.104843
Abstract: In contrast to ancient Western and Asian cultures, medicinal plants of the Aboriginal and Torres Strait Islanders in Australia have not been as intensively studied for their molecular composition and molecular bioactivity. Syncarpia glomulifera subsp.… read more here.
Keywords: anti inflammatory; syncarpia glomulifera; tetragocarbone sideroxylin; potent anti ... See more keywords
Pyridobenzothiazolones Exert Potent Anti-Dengue Activity by Hampering Multiple Functions of NS5 Polymerase.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.9b00619
Abstract: Treatment of dengue virus (DENV) and other flavivirus infections is an unmet medical need. The highly conserved flaviviral NS5 RNA-dependent RNA polymerase (RdRp) is an attractive antiviral target that interacts with NS3 and viral RNA… read more here.
Keywords: anti dengue; potent anti; exert potent; polymerase ... See more keywords
Identification of novel furo[2,3-d]pyrimidine based chalcones as potent anti-breast cancer agents: synthesis, in vitro and in vivo biological evaluation
Sign Up to like & getrecommendations! Published in 2022 at "RSC Advances"
DOI: 10.1039/d2ra00889k
Abstract: Various substituted synthetic chalcones demonstrated potent anti-cancer activities. In the current study a series of novel furo[2,3-d]pyrimidine based chalcones were synthesized as potential anticancer agents. Among the different substituted derivatives, two of the halogen bearing… read more here.
Keywords: novel furo; based chalcones; potent anti; pyrimidine based ... See more keywords
Virus-like particle display of HER2 induces potent anti-cancer responses
Sign Up to like & getrecommendations! Published in 2018 at "Oncoimmunology"
DOI: 10.1080/2162402x.2017.1408749
Abstract: ABSTRACT Overexpression of human epidermal growth factor receptor-2 (HER2) occurs in 20–30% of invasive breast cancers. Monoclonal antibody therapy is effective in treating HER2-driven mammary carcinomas, but its utility is limited by high costs, side… read more here.
Keywords: like particle; potent anti; virus like; cancer ... See more keywords
Potent anti-tumor activity of CD45RA-targeting Hm3A4-Ranpirnase against myeloid lineage leukemias
Sign Up to like & getrecommendations! Published in 2022 at "Bioengineered"
DOI: 10.1080/21655979.2022.2054159
Abstract: ABSTRACT CD45RA is a specific marker for leukemia stem cell (LSC) sub-populations in acute myeloid leukemia (AML). Ranpirnase (Rap), an amphibian RNase, has been extensively investigated in preclinical and clinical studies for its antitumor activity.… read more here.
Keywords: immunotoxin; activity; potent anti; rap ... See more keywords
Δ8‐Tetrahydrocannabivarin has potent anti‐nicotine effects in several rodent models of nicotine dependence
Sign Up to like & getrecommendations! Published in 2019 at "British Journal of Pharmacology"
DOI: 10.1111/bph.14844
Abstract: Both types of cannabinoid receptors—CB1 and CB2—regulate brain functions relating to addictive drug‐induced reward and relapse. CB1 receptor antagonists and CB2 receptor agonists have anti‐addiction efficacy, in animal models, against a broad range of addictive… read more here.
Keywords: potent anti; nicotine effects; effects several; anti nicotine ... See more keywords
Pharmacological Activation of STING in Bladder Induces Potent Anti-tumor Immunity in Non-Muscle Invasive Murine Bladder Cancer.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular cancer therapeutics"
DOI: 10.1158/1535-7163.mct-21-0780
Abstract: Schweinfurthins, a class of natural products, have attracted considerable interest for novel therapy development because of their selective and potent anti-proliferative activity against human cancer cells. However, the underlying mechanism is not well understood. Herein,… read more here.
Keywords: bladder; activation; mtor akt; potent anti ... See more keywords
Abstract 160: High target binding affinity with long lasting cellular target engagement and high dose intermittent schedule of PI3K inhibitor copanlisib contribute to the potent anti-tumor activity and good safety profile
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-160
Abstract: Introduction: Several generations of PI3K inhibitors have been tested in clinic. However, thus far, clinical activity has been moderate. Different from other oral PI3K inhibitors dosed continuously, copanlisib (BAY 80-6946) is an intravenous PI3K inhibitor… read more here.
Keywords: pi3k; affinity; potent anti; target ... See more keywords