A5061704800- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthesis and biological activity
- Click Chemistry and Applications
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis of β-Lactam Compounds
- Synthesis and Biological Evaluation
- Cancer therapeutics and mechanisms
- Synthesis and Biological Activity
- Phytochemistry and Biological Activities
- Quinazolinone synthesis and applications
- Synthesis and Catalytic Reactions
- Crystallography and molecular interactions
- Synthesis of Tetrazole Derivatives
- Computational Drug Discovery Methods
- Bioactive Compounds and Antitumor Agents
- Microbial Natural Products and Biosynthesis
- Curcumin's Biomedical Applications
- Cholinesterase and Neurodegenerative Diseases
- Drug-Induced Hepatotoxicity and Protection
- Colorectal Cancer Treatments and Studies
- Cancer Treatment and Pharmacology
- Enzyme function and inhibition
- Biochemical and Molecular Research
- Research on Leishmaniasis Studies
King Abdulaziz University
2019-2025
Trinity College Dublin
2015-2022
Virginia Commonwealth University
2020
Semisynthetic modifications of natural products have bestowed us with many anticancer drugs. In the present work, a product, eugenol, has been modified synthetically to generate new agents. The final compounds were structurally confirmed by NMR, IR, and mass techniques. From cytotoxicity results, compound 17 bearing morpholine was found be most active cytotoxic agent IC50 1.71 (MCF-7), 1.84 (SKOV3), 1.1 μM (PC-3) thymidylate synthase (TS) inhibitor an 0.81 μM. Further cellular studies showed...
Thymidylate synthase (TS) has emerged as a hot spot in cancer treatment, it is directly involved DNA synthesis. In the present article, nine hybrids containing 1,2,3-triazole and 1,3,4-oxadiazole moieties (6-14) were synthesized evaluated for anticancer vitro thymidylate activities. According to silico pharmacokinetic studies, exhibited good drug likeness properties bioavailability. The cytotoxicity results indicated that compounds 12 13 remarkable inhibition on tested Michigan Cancer...
A library of novel naproxen based 1,3,4-oxadiazole derivatives (8–16 and 19–26) has been synthesized screened for cytotoxicity as EGFR inhibitors. Among the hybrids, compound2-(4-((5-((S)-1-(2-methoxynaphthalen-6-yl)ethyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)phenol(15) was most potent compound against MCF-7 HepG2cancer cells with IC50 2.13 1.63 µg/mL, respectively, equipotent to doxorubicin (IC50 1.62 µg/mL) towards HepG2. Furthermore, 15 inhibited kinase 0.41 μM compared...
A library of 1,2,3-triazole-incorporated thymol-1,3,4-oxadiazole derivatives (6–18) hasbeen synthesized and tested for anticancer antimicrobial activities. Compounds 7, 8, 9, 10, 11 exhibited significant antiproliferative activity. Among these active derivatives, compound 2-(4-((5-((2-isopropyl-5-methylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)phenol (9) was the best against all three cell lines, MCF-7 (IC50 1.1 μM), HCT-116 2.6 HepG2 1.4 μM). Compound 9 found to...
Here, we synthesized a newseries of mono- and bis(dimethylpyrazolyl)-s-triazine derivatives. The synthetic methodology involved the reaction different dihydrazinyl-s-triazine derivatives with acetylacetone in presence triethylamine to produce corresponding target products high yield purity. antiproliferative activity novel was studied against three cancer cell lines, namely, MCF-7, HCT-116, HepG2. N-(4-Bromophenyl)-4-(3,5-dimethyl-1H-pyrazol-1-yl)-6-morpholino-1,3,5-triazin-2-amine 4f,...
The combination of lopinavir/ritonavir remains one the first-line therapies for initial antiretroviral regimen in pediatric HIV-infected children. However, implementation this recommendation has faced many challenges due to cold-chain requirements, high alcohol content, and unpalatability ritonavir-boosted lopinavir syrup. In addition, administration crushed tablets shown a detriment oral bioavailability both drugs. Therefore, there is clinical need develop safer better formulations adapted...
Andrographolide (AG), a major active constituent of Andrographis paniculata, is known to hinder proliferation several types cancer cells. However, its poor solubility and cellular permeability restrict use in clinical applications. In this study, AG-loaded phytosomes (AG-PTMs) were formulated optimized with respect particle size using l-α-phosphatidylcholine (PC):AG ratio sonication time (ST) as independent variables. The formula was prepared at 1:2.7 for AG:PC molar 4.9 min ST exhibited...
All the previously reported phenylpyrazoles as carbonic anhydrase inhibitors (CAIs) were found to have small sizes and high levels of flexibility, hence showed low selectivity profiles toward a particular isoform CA. Herein, we report development more rigid ring system bearing sulfonamide hydrophilic head lipophilic tail develop novel molecules that are suggested better special CA isoform. Accordingly, three sets pyrano[2,3-c]pyrazoles attached with aryl hydrophobic synthesized enhance...
Structure–activity relationships for a series of 3-phenoxy-1,4-diarylazetidin-2-ones were investigated, leading to the discovery number potent antiproliferative compounds, including trans-4-(3-hydroxy-4-methoxyphenyl)-3-phenoxy-1-(3,4,5-trimethoxyphenyl)azetidin-2-one (78b) and trans-4-(3-amino-4-methoxyphenyl)-3-phenoxy-1-(3,4,5-trimethoxyphenyl)azetidin-2-one (90b). X-ray crystallography studies indicate potential importance torsional angle between 1-phenyl “A” ring 4-phenyl “B” activity...
We report the preparation and cytotoxicity of two new eugenol derivatives that contain 1,3,4-oxadiazole, as novel inhibitors thymidylate synthase; these are shown to be promising chemotherapeutic agents.
Background/Objectives: The synthesis of (E)-1-(1,3-diphenylallyl)-1H-1,2,4-triazoles and related compounds as anti-mitotic agents with activity in breast cancer was investigated. These were designed hybrids the microtubule-targeting chalcones, indanones, aromatase inhibitor letrozole. Methods: A panel 29 synthesized examined by a preliminary screening estrogen receptor (ER) progesterone (PR)-positive MCF-7 cells together cell cycle analysis tubulin polymerization inhibition. Results:...
A series of novel 1,4-diaryl-2-azetidinone analogues combretastatin A-4 (CA-4) have been designed, synthesised and evaluated in vitro for antiproliferative activity, antiapoptotic activity inhibition tubulin polymerisation. Glucuronidation CA-4 by uridine 5-diphosphoglucuronosyl transferase enzymes (UGTs) has identified as a mechanism resistance cancer cells. Potential sites ring B glucuronate conjugation are removed replacing the meta-hydroxy substituent selected β-lactams with alternative...
A new series of quinoline derivatives combretastatin A-4 have been designed, synthesised and demonstrated as tubulin polymerisation inhibitors. These novel compounds showed significant antiproliferative activities, among them,
The membrane-bound human carbonic anhydrase (hCA) IX is widely recognized as a marker of tumor hypoxia and prognostic factor within several cancers. Being undetected in most normal tissues, hCA-IX implies the pharmacotherapeutic advent reduced off-target adverse effects. We assessed potential anticancer activity bumetanide-based analogues to inhibit enzymatic cell proliferation two solid cancer lines, namely kidney carcinoma (A-498) bladder squamous (SCaBER). Bumetanide efficiently target...
A novel series of quinoline derivatives combretastatin A-4 incorporating rigid hydrazone and a cyclic oxadiazole linkers were synthesized have demonstrated potent tubulin polymerization inhibitory properties. Many these shown significant antiproliferative activities in the submicromolar range. The most compound, 19h, superior IC50 values ranging from 0.02 to 0.04 µM against four cancer cell lines while maintaining low cytotoxicity MCF-10A non-cancer cells, thereby suggesting 19h’s...
Lepidium sativum seeds are used traditionally to accelerate healing of bone fracture in addition its culinary uses. This study aimed characterize the osteoprotective effect L. an ovariectomized rat model at two dose levels (50 and 100 mg/kg) using 17β-estradiol as a positive reference standard. Moreover, complete metabolite profile via UHPLC/PDA/ESI–MS, well headspace solid-phase microextraction (SPME)-GC/MS is presented. Results revealed that extract exhibited significant anti-osteoporotic...
Based on the use of s-triazine as a scaffold, we report here new series Schiff base derivatives and their anti-proliferative activity against two cancer cell lines: human breast carcinoma (MCF-7), colon (HCT-116) compared with tamoxifen reference compound. Several exhibited growth inhibition in sub-micromolar range. The results reveal that showed varied activities substituents core have great effect activity. Compounds piperidino benzylamino substituent moiety 4b 4c were most effective both...
Recently, combining histone deacetylase (HDAC) inhibitors with chemotherapeutic drugs or agents, in particular epidermal growth factor receptor (EGFR) inhibitors, is considered to be one of the most encouraging strategy enhance efficacy antineoplastic agents and decrease avoid drug resistance. Therefore, this work, based on introducing 3,4,5-trimethoxy phenyl group as a part CAP moiety, addition incorporating 4–6 aliphatic carbons linker using COOH hydroxamic acid ZBG, 12 novel EGFR/HDAC...