A5005819098- Synthesis and biological activity
- Click Chemistry and Applications
- Synthesis and Biological Evaluation
- Cancer therapeutics and mechanisms
- Malaria Research and Control
- HIV/AIDS drug development and treatment
- Synthesis and Catalytic Reactions
- Genomics and Chromatin Dynamics
- Protein Degradation and Inhibitors
- Bioactive Compounds and Antitumor Agents
- Synthesis and bioactivity of alkaloids
- PARP inhibition in cancer therapy
- Computational Drug Discovery Methods
- Carbohydrate Chemistry and Synthesis
- Synthesis of β-Lactam Compounds
- Cancer Genomics and Diagnostics
- Drug Transport and Resistance Mechanisms
- Ferrocene Chemistry and Applications
- Natural Antidiabetic Agents Studies
- Lysosomal Storage Disorders Research
- Natural Compounds in Disease Treatment
- Phenothiazines and Benzothiazines Synthesis and Activities
- Crystallization and Solubility Studies
- Cancer, Lipids, and Metabolism
- DNA Repair Mechanisms
University of KwaZulu-Natal
2018-2024
University of Montana
2022-2024
University of Colorado Anschutz Medical Campus
2023-2024
Center for Discovery
2023-2024
University of Colorado Denver
2022
University of Colorado Cancer Center
2022
University of Zululand
2021
University of Ibadan
2014
Diabetes mellitus (DM) is a multifaceted metabolic disorder that remains major threat to global health security. Sadly, the clinical relevance of available drugs burdened with an upsurge in adverse effects; hence, inhibiting carbohydrate-hydrolyzing enzymes α-glucosidase and α-amylase while preventing oxidative stress deemed practicable strategy for regulating postprandial glucose levels DM patients. We report herein inhibition antioxidant profile quinoline hybrids 4a-t 12a-t bearing...
Two libraries of quinoline-based hybrids 1-(7-chloroquinolin-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine and 7-chloro-N-phenylquinolin-4-amine were synthesized evaluated for their α-glucosidase inhibitory antioxidant properties. Compounds with 4-methylpiperidine para-trifluoromethoxy groups, respectively, showed the most promising inhibition activity IC
Abstract A library of novel pyrazole–imidazo[1,2‐α]pyridine scaffolds was designed and synthesized through a one‐pot three‐component tandem reaction. The structures conjugates were confirmed by spectroscopic techniques (NMR, IR HRMS). In vitro antibacterial evaluation the twelve molecules ( 7a , 8a–k ) against methicillin‐resistant Staphylococcus aureus normal strains Escherichia coli Salmonella typhimurium Klebsiella pneumonia Pseudomonas aeruginosa established 8b 8d 8e 8h 8i as potent...
Abstract A series of coumarin‐tagged β ‐lactam triazole hybrids ( 10a – 10o ) were synthesized and tested for their cytotoxic activity against MDA‐MB‐231 (triple negative breast cancer), MCF‐7 (estrogen receptor positive cancer (ER+)) A549 (human lung carcinoma) cell lines including one normal line, HEK‐293 embryonic kidney). Two compounds 10b 10d exhibited substantial effect with IC 50 values 53.55 58.62 μ m , respectively. More importantly, non‐cytotoxic lines. Structure–activity...
Oil was extracted from the seed of Hura crepitans using hexane in a soxhlet extractor and analyzed for iodine value, saponification value free fatty acid content. The dominant oil C18:2 (<mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML" id="M1"><mml:mn>52.8</mml:mn><mml:mo>±</mml:mo><mml:mn>0.10</mml:mn></mml:math>%) while <mml:math id="M2"><mml:mn>120.10</mml:mn><mml:mo>±</mml:mo><mml:mn>0.70</mml:mn></mml:math> g iodine/100 g. Biodiesel produced two-step reaction system involving...
A series of 1<italic>H</italic>-1,2,3 triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates were synthesized and <italic>in vitro</italic> evaluated against estrogen responsive (MCF-7) triple negative (MDA-MB-231) breast cancer cells.
Aim: WHO Malaria report 2017 estimated 216 million cases of malaria and 445,000 deaths worldwide, with 91% affecting the African region. Results/methodology: Microwave promoted synthesis cycloalkyl amine substituted isoindoline-1,3-dione-4-aminoquinolines was urbanized for evaluating their antiplasmodial activities. Compound optimum combination propyl chain length hydroxyethyl piperazine proved to be most potent among synthesized scaffolds against chloroquine-resistant W2 strain Plasmodium...
The Chromodomain helicase DNA-binding protein 1-like (CHD1L) is a nucleosome remodeling enzyme, which plays key role in chromatin relaxation during the DNA damage response. Genome editing has shown that deletion of CHD1L sensitizes cells to PARPi, but effect its pharmacological inhibition not been defined. Triple-negative breast cancer SUM149PT, HCC1937, and MDA-MB-231 were used assess mechanism action CHD1Li OTI-611. Cytotoxicity as single agent or combination with standard-of-care...
A series of naphthalimide-chalcone/pyrazoline conjugates was prepared and evaluated for their anti-breast cancer potential against estrogen responsive, i.e. MCF-7 (ER+), triple-negative, MDA-MB-231 (ER-), cell lines. The structure-activity-relationship (SAR) deduced based on the influence linker length, substituents phenyl ring generated functionalities, anti-proliferative activities. Docking simulations further delineate type interactions designed molecules with selected targets. This...
A series of amide tethered 4-aminoquinoline-naphthalimide hybrids has been synthesized to assess their in vitro antiplasmodial potential against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains Plasmodium falciparum. The most active noncytotoxic compound had an IC50 value 0.07 μM W2 strain was more than standard antimalarial drugs, including chloroquine, desethylamodiaquine, quinine, particularly for drug resistant malaria. promising scaffold, when subjected heme binding...
Chromodomain helicase DNA-binding protein 1 like (CHD1L) is an oncogene implicated in tumor progression, multidrug resistance, and metastasis many types of cancer. In this article, we described the optimization first lead CHD1L inhibitors (CHD1Li) through drug design medicinal chemistry. More than 30 CHD1Li were synthesized evaluated using a variety colorectal cancer (CRC) organoid models functional assays. The results led to prioritization six analogues with improved potency, antitumor...
The persistence of breast cancer as the leading cause mortality among women, coupled with drug resistance to tamoxifen, standard endocrine therapy for disease, exacts continuous attention. To this effect, molecular hybridisation offers an attractive route drugs improved bioactivity profiles.The primary goal study was examine potential 1H-1,2,3-triazole linked quinolineisatin hybrids candidates against and Methicillin-Resistant Staphylococcus aureus (MRSA) cells.The quinoline-isatin were...
Malaria parasites continue to pose a concern. Drug resistance underlines the need for new structural cores that, when combined with existing antimalarial frameworks, can partially re-sensitize drug-resistant available drugs, such as chloroquine (CQ). Herein, we used "covalent biotherapy" design and synthesize series of aminoquinoline-oxindoles. The most promising hybrid exhibited an IC50 value 30.9 nM against W2 strain P. falciparum, was seven-fold more active than CQ. To decipher mode...
Transient receptor potential ankyrin 1 (TRPA1) protein plays an important role in the inflammatory response, and it has been associated with different pain conditions pain-related diseases, making TRPA1 a valid target for painkillers. In this study, we identified inhibitors located their binding sites utilizing computer-aided drug design (CADD) techniques. The designed 3-phenylcoumarin-based were successfully synthesized using microwave assisted synthetic strategy....
A new library of quinoline–natural product conjugates bearing 1,2,3-triazole moiety as a linker has been synthesized using the copper(I) catalyzed azide-alkyne [3 + 2] cycloaddition reaction (CuAAC) methodology. The structure characterization compounds was achieved NMR and HRMS analysis. were subsequently screened for their antimicrobial efficacies against methicillin resistant Staphylococcus aureus (MRSA), MDR Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa,...
Colorectal cancer (CRC) is one of the most prevalent and deadly forms cancer. It universally treated with a combination DNA damaging chemotherapy drugs irinotecan, 5-Fluorouracil (5-FU), oxaliplatin.