A5032954885- Synthesis and biological activity
- Synthesis and Characterization of Heterocyclic Compounds
- Click Chemistry and Applications
- Adenosine and Purinergic Signaling
- Receptor Mechanisms and Signaling
- Synthesis and Biological Evaluation
- Pharmacological Receptor Mechanisms and Effects
- Quinazolinone synthesis and applications
- Microtubule and mitosis dynamics
- Synthesis of heterocyclic compounds
- Plant Ecology and Soil Science
- Redox biology and oxidative stress
- Lung Cancer Research Studies
- Genomics, phytochemicals, and oxidative stress
- Soil and Land Suitability Analysis
- Angiogenesis and VEGF in Cancer
- Accounting and Financial Management
- Heat shock proteins research
- Photochromic and Fluorescence Chemistry
- Synthesis of Organic Compounds
- ATP Synthase and ATPases Research
- Biochemical Analysis and Sensing Techniques
- Proteoglycans and glycosaminoglycans research
- Bioactive Compounds and Antitumor Agents
- Advanced Materials Characterization Techniques
National Institute of Diabetes and Digestive and Kidney Diseases
2021-2024
National Institutes of Health
2021-2024
University of Ferrara
2016-2022
University of Basel
2020
The clinical evidence for the success of tyrosine kinase inhibitors in combination with microtubule-targeting agents prompted us to design and develop single that possess both epidermal growth factor receptor (EGFR) tubulin polymerization inhibitory properties. A series 6-aryl/heteroaryl-4-(3′,4′,5′-trimethoxyanilino)thieno[3,2-d]pyrimidine derivatives were discovered as novel dual EGFR inhibitors. 4-(3′,4′,5′-trimethoxyanilino)-6-(p-tolyl)thieno[3,2-d]pyrimidine derivative 6g was most...
Abstract A novel series of tubulin polymerization inhibitors, based on the 1-(3′,4′,5′-trimethoxyphenyl)-2-aryl-1 H -imidazole scaffold and designed as cis -restricted combretastatin A-4 analogues, was synthesized with goal evaluating effects various patterns substitution phenyl at 2-position imidazole ring biological activity. chloro ethoxy group meta - para -positions, respectively, produced most active compound in ( 4o ), IC 50 values 0.4-3.8 nM against a panel seven cancer cell lines....
We recently reported N4-substituted 3-methylcytidine-5′-α,β-methylenediphosphates as CD73 inhibitors, potentially useful in cancer immunotherapy. now expand the structure–activity relationship of pyrimidine nucleotides human inhibitors. 4-Chloro (MRS4598 16; Ki = 0.673 nM) and 4-iodo (MRS4620 18; 0.436 substitution N4-benzyloxy group decreased by ∼20-fold. Primary alkylamine derivatives coupled through a p-amido with varying methylene chain length (24 25) were functionalized congeners, for...
Abstract Antimitotic agents that interfere with microtubule formation are one of the major classes cytotoxic drugs for cancer treatment. Multiple 2-methyl-4-(3′,4′,5′-trimethoxyphenyl)-5-substituted oxazoles and their related 4-substituted-5-(3′,4′,5′-trimethoxyphenyl) regioisomeric derivatives designed as cis -constrained combretastatin A-4 (CA-4) analogues were synthesized evaluated antiproliferative activity in vitro against a panel cell lines and, selected highly active compounds,...
Two different series of fifty-two compounds, based on 3′,4′,5′-trimethoxyaniline (7a–ad) and variably substituted anilines (8a–v) at the 7-position 2-substituted-[1,2,4]triazolo [1,5-a]pyrimidine nucleus, had moderate to potent antiproliferative activity against A549, MDA-MB-231, HeLa, HT-29 Jurkat cancer cell lines. All derivatives with a common 3-phenylpropylamino moiety 2-position triazolopyrimidine scaffold halogen-substituted its 7-position, corresponding 4′-fluoroaniline (8q),...
(1) Background: In the development of new and more effective anticancer approaches, combined treatments appear great interest. Combination therapy could be importance in management glioblastoma (GBM), a lethal malignancy that accounts for 42% cancer central nervous system, with median survival 15 months. This study aimed to verify activity on cell line one most active compounds novel series tubulin polymerization inhibitors based 1-(3',4',5'-trimethoxyphenyl)-2-aryl-1H-imidazole scaffold,...
A further investigation aiming to generate new potential antitumor agents led us synthesize a series of twenty-two compounds characterized by the presence 7-(3',4',5'-trimethoxyphenyl)-[1,2,4]triazolo[1,5-
Two novel series of compounds based on the 4,5,6,7-tetrahydrothieno[2,3-c]pyridine and 4,5,6,7-tetrahydrobenzo[b]thiophene molecular skeleton, characterized by presence a 3′,4′,5′-trimethoxyanilino moiety cyano or an alkoxycarbonyl group at its 2- 3-position, respectively, were designed, synthesized, evaluated for antiproliferative activity panel cancer cell lines selected highly active compounds, inhibition tubulin polymerization, cycle effects. We have identified...
The World Health Organization reported that approximately 324,000 new cases of melanoma skin cancer were diagnosed worldwide in 2020. incidence has been increasing over the past decades. Targeting apoptotic pathways is a potential therapeutic strategy transition to preclinical models and clinical trials. Some naturally occurring products synthetic derivatives are apoptosis inducers may represent realistic option fight against disease. Thus, chalcones have received considerable attention due...
The combination of two pharmacophores into a single molecule represents one the methods that can be adopted for synthesis new anticancer molecules. To investigate influence position pyridine nitrogen on biological activity, different series α-bromoacryloylamido indolyl pyridinyl propenones 3a–h and 4a–d were designed synthesized by pharmacophore hybridization approach evaluated their antiproliferative activity against panel six human cancer cell lines. These hybrid molecules prepared to...
In the development of novel and more effective anticancer approaches, combined treatments appear to be great interest, based on possibility obtaining relevant biological or therapeutic effects using lower concentrations single drugs. Combination therapy may prove utmost significance in management glioblastoma (GBM), a lethal malignancy that accounts for 42% cancer cases central nervous system, with median survival rate 15 months. As regards authors have recently demonstrated peptide nucleic...
Abstract Tubulin binding agents (TBAs) are commonly used in cancer therapy as antimitotics. It has been described that TBAs, like combretastatin A-4 (CA-4), present also antivascular activity and among its derivatives we identified TR-764 a new inhibitor of tubulin polymerization, based on the 2-(alkoxycarbonyl)-3-(3′,4′,5′-trimethoxyanilino)benzo[ b ]thiophene molecular skeleton. The antiangiogenic (1–10 nM) was tested vitro human umbilical endothelial cells (HUVECs) vivo , chick embryo...
Polo-like kinase 1 (Plk1) is considered an attractive target for anticancer therapy. Over the years, studies on noncatalytic polo-box domain (PBD) of Plk1 have raised expectation generating highly specific protein–protein interaction inhibitors. However, molecular nature canonical PBD-dependent interaction, which requires extensive water network–mediated interactions with its phospholigands, has hampered efforts to identify small molecules suitable PBD drug discovery. Here, we report...