A5064918006- Plant-based Medicinal Research
- Bioactive Natural Diterpenoids Research
- Advanced Synthetic Organic Chemistry
- Alkaloids: synthesis and pharmacology
- Cancer Treatment and Pharmacology
- Berberine and alkaloids research
- Synthetic Organic Chemistry Methods
- Inflammatory mediators and NSAID effects
- Synthesis and biological activity
- Curcumin's Biomedical Applications
- Silymarin and Mushroom Poisoning
- Synthesis and Characterization of Heterocyclic Compounds
- Traditional Chinese Medicine Analysis
- Cholinesterase and Neurodegenerative Diseases
- Synthesis and bioactivity of alkaloids
- Ubiquitin and proteasome pathways
- Chemical synthesis and alkaloids
- Pharmacological Effects of Natural Compounds
- Computational Drug Discovery Methods
- Synthesis and Reactions of Organic Compounds
- Prostate Cancer Treatment and Research
- Synthesis and Biological Activity
- Asymmetric Hydrogenation and Catalysis
- Synthesis and Biological Evaluation
- Bioactive Compounds and Antitumor Agents
Virginia Tech
2008-2025
California State University, Fresno
2015-2024
Xinjiang Academy of Agricultural and Reclamation Science
2022
Fujian Medical University
2020
California State University System
2019
Zhejiang Sci-Tech University
2013-2017
Sichuan University
2003-2014
Sichuan Agricultural University
2012
Emory University
2010
University of Alberta
2005-2008
Induced protein degradation has emerged as an innovative drug discovery approach, complementary to the classical method of suppressing function. The androgen receptor signaling pathway been identified primary driving force in development and progression lethal castration-resistant prostate cancer. Since degraders function differently from antagonists, they hold promise overcome resistance challenges faced by current therapeutics. Proteolysis-targeting chimeras (PROTACs), monomeric degraders,...
Bioassay-guided fractionation of an n-BuOH extract the lateral roots Aconitum carmichaeli. led to isolation 5 cardioactive C19-diterpenoid alkaloids: N-deethylaconine (1), beiwutinine (2), hypaconine (3), mesaconine (4), and 15α-hydroxyneoline (5). N-Deethylaconine are new aconitine-type alkaloids. Hypaconine was isolated from this species for first time. Among them, mesaconine, hypaconine, showed strongest cardiac actions on perfused bullfrog heart. Furthermore, has protective effects,...
Forty-three 1,5-diheteroaryl-1,4-pentadien-3-ones were designed as potential curcumin mimics, structurally featuring a central five-carbon dienone linker and two identical nitrogen-containing aromatic rings. They synthesized using Horner-Wadsworth-Emmons reaction the critical step evaluated for their cytotoxicity antiproliferative activities toward both androgen-insensitive androgen-sensitive prostate cancer cell lines an aggressive cervical line. Most of compounds showed distinctly better...
Abstract Background The Old World sand fly, Phlebotomus papatasi (Scopoli), a vector of zoonotic cutaneous leishmaniasis, is usually controlled by insecticides, including anticholinesterases. Previous studies have revealed 85% amino acid sequence identity recombinant P. acetylcholinesterase (r Pp AChE1) to mosquito AChE. They identified synthetic carbamates that selectively inhibited r AChE1 and circumvented the G119S mutation responsible for high-level resistance This study reports...
A group of 1,3-diarylprop-2-yn-1-ones (13, 17, 23, 26 and 27) possessing a C-3 p-SO2Me COX-2 pharmacophore were designed, synthesized evaluated as potential dual inhibitors cyclooxygenase-1/2 (COX-1/2) 5/15-lipoxygenases (5/15-LOX) that exhibit vivo antiinflammatory analgesic activities. Among this class compounds, 3-(4-methanesulfonylphenyl)-1-(4-fluorophenyl)prop-2-yn-1-one (13h) was identified potent selective inhibitor (COX-2 IC50 = 0.1 μM; SI 300), being 5-fold more than rofecoxib 0.5 >...
The carboxylic acid group of the anti-inflammatory (AI) drugs aspirin and indomethacin was covalently linked to 1-(2-carboxypyrrolidin-1-yl)diazen-1-ium-1,2-diolate ion via a one-carbon methylene spacer obtain two new hybrid prodrugs. prodrug (23) 2.2-fold more potent AI agent than aspirin, whereas (26) about 1.6-fold less indomethacin. Prodrugs 23 26 slowly released nitric oxide (NO) upon dissolution in phosphate buffer at pH 7.4 (1.1 mol NO/mol compound after 43 h), but rate extent NO...
For evaluation of C18- and C19-diterpenoid alkaloids as analgesics, three were isolated from the roots Aconitum hemsleyanum var. circinatum A. transsecutum; twenty-five semisynthetic or prepared lappaconitine, crassicauline A yunaconitine. In a mice acetic acid-induced abdominal constriction assay, four analogs yunaconitine exhibited good analgesic activities with 77.8—94.1% inhibition range in 0.1—10 mg/kg subcutaneous (s.c.) dose at point 20 min after drug administration. Among them,...
A convergent and efficient formal synthesis of (±)-atisine has been accomplished. The synthetic strategy is to efficiently construct the bicyclo[2.2.2]octane ring moiety by an oxidative dearomatization/intramolecular Diels-Alder cycloaddition cascade. first total another atisine-type C(20)-diterpenoid alkaloid, (±)-isoazitine, also achieved employing same strategy.
Curcumin is a biologically active polyphenol that exists in Indian spice turmeric. It has been reported curcumin exerted anti-inflammatory, anti-oxidant and anti-cancer effects numerous vitro vivo studies. However, it not well-understood the molecular mechanism of for cancer stem cells telomerase colorectal cancer. In this study, compound 19, nitrogen-containing analog, was used to treat human cells. Compound 19 showed greater anti-proliferative activity than while displayed no significant...
ADVERTISEMENT RETURN TO ISSUEPREVBook ReviewNEXTReview of Chemical Synthesis Hormones, Pheromones and Other BioregulatorsQiao-Hong ChenView Author Information Virginia TechBlacksburg, VirginiaCite this: J. Nat. Prod. 2011, 74, 7, 1671Publication Date (Web):June 23, 2011Publication History Published online23 June 2011Published inissue 22 July 2011https://pubs.acs.org/doi/10.1021/np200497hhttps://doi.org/10.1021/np200497hbook-reviewACS PublicationsCopyright © 2011 The American Society...
Acetylcholinesterase (AChE) is a proven target for control of the malaria mosquito (Anopheles gambiae). Unfortunately, single amino acid mutation (G119S) in An. gambiae AChE-1 (AgAChE) confers resistance to AChE inhibitors currently approved by World Health Organization indoor residual spraying. In this report, we describe several carbamate that potently inhibit G119S AgAChE and are contact-toxic carbamate-resistant gambiae. PCR-RFLP analysis was used confirm carbamate-susceptible G3 Akron...