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Novel 8-Methoxycoumarin-3-Carboxamides with potent anticancer activity against liver cancer via targeting caspase-3/7 and β-tubulin polymerization
In the present study, we explored the potential of coumarin-based compounds, known for their potent anticancer properties, by designing and...
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Cu(II)-bis(benzoylacetonate) complexes as potential inhibitors for tubulin polymerization: synthesis, crystal structure, spectral characterization, HSA, DFT, molecular docking studies, and antioxidant activity
The reaction of 1-phenyl-1,3-butanedione, also known as benzoylacetone (bzac), with adequate copper salts (sulfate/acetate) at a molar ratio of 2:1...
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Pyrazoles, isoxazoles, and 1,2,3-triazoles as analogs of the natural cytostatic combretastatin A-4: efficient routes of synthesis, tubulin inhibition, and cytotoxicity
The review discusses the advantages and disadvantages of combretastatin A-4, presents the most effective methods for the synthesis of its...
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Cytotoxic mechanism of tioconazole involves cell cycle arrest at mitosis through inhibition of microtubule assembly
Tioconazole is one of the drugs used to treat topical mycotic infections. It exhibited severe toxicity during systemic administration; however, the...
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Heterocycles from Cyanobacteria
Targets of cyanobacterial heterocyclic cytotoxins classify into tubulin, actin, and the sodium channel. In addition, cyanobacteria produce...
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Disruption of alpha-tubulin releases carbon catabolite repression and enhances enzyme production in Trichoderma reesei even in the presence of glucose
BackgroundTrichoderma reesei is a filamentous fungus that is important as an industrial producer of cellulases and hemicellulases due to its high...
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C(7)-Derivatives of colchicine with guanosine and biphenyl moieties: molecular modeling, synthesis, and tubulin clustering effect in cancer cells
Two novel C(7)-derivatives of natural anticancer agent colchicine were designed with the purpose to study their ability to induce tubulin clustering...
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Chemical Biology Studies on Aplyronine A, A PPI-Inducing Antitumor Macrolide from Sea Hare
The antitumor macrolide aplyronine A (ApA) disturbs microtubule (MT) dynamics by inducing the protein–protein interaction (PPI) between actin and...
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SIRT1 deacetylates WEE1 and sensitizes cancer cells to WEE1 inhibition
The cell-cycle checkpoint kinase WEE1 is emerging as a therapeutic target for cancer treatment. However, how its catalytic activity is regulated...
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Synthesis of Biologically Active Heterocyclic Stilbene and Chalcone Analogs of Combretastatin
Combretastatin A-4 (CA-4, 7) has had a major impact in the field of medicinal chemistry as a potent bioactive molecule that binds to the...
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Pharmacological inhibition of Kir4.1 evokes rapid-onset antidepressant responses
Major depressive disorder, a prevalent and severe psychiatric condition, necessitates development of new and fast-acting antidepressants. Genetic...
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LNX2 involves in the role of ghrelin to promote the neuronal differentiation of adipose tissue-derived mesenchymal stem cells
Adipose tissue-derived mesenchymal stem cells (ADSCs) have promising effects on nerve repair due to the differentiation ability to neural cells....
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New record of reusing brewing by-product for biosynthesis of prodigiosin and its novel anti-pathogen fungi via in vitro tests and molecular docking study
Prodigiosin (PG)—a molecule with promising applications in many fields—was effectively biosynthesized in this study using a novel and eco-friendly...
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GSK-3β suppression upregulates Gli1 to alleviate osteogenesis inhibition in titanium nanoparticle-induced osteolysis
Wear particle-induced periprosthetic osteolysis (PPO) have become a major reason of joint arthroplasty failure and secondary surgery following joint...
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Colchicine delivered by a novel nanoparticle platform alleviates atherosclerosis by targeted inhibition of NF-κB/NLRP3 pathways in inflammatory endothelial cells
Atherosclerosis, a chronic inflammatory disease characterized by arterial plaque formation, is one of the most prominent causes of cardiovascular...
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Development of 9-(N-arylmethylamino) congeners of noscapine: the microtubule targeting drugs for the management of breast cancer
Noscapine is a natural lead molecule with anticancer activity at a higher concentrations. So, there is an urge for the development of more potent...
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Xanthatin and 8-epi-xanthatin as new potential colchicine binding site inhibitors: a computational study
ContextPhytocompounds xanthatin and 8- epi -xanthatin, obtained from Xanthium chinese Mill , showed antitumoral activity in vitro related to the...
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Role of structural components of the 2-methoxyestradiol—chlorambucil conjugate in microtubule stabilization
The conjugate of 2-methoxyestradiol, a ligand for the cell protein tubulin, with two molecules of chlorambucil, known as a DNA-alkylating agent, is...
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Noscapinoids: A Family of Microtubule-Targeted Anticancer Agent
Noscapine (C22H23NO7), benzylisoquinoline alkaloid was reported to bind tubulin, limiting the process of division of cells at mitosis without...
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A divergent intermediate strategy yields biologically diverse pseudo-natural products
The efficient exploration of biologically relevant chemical space is essential for the discovery of bioactive compounds. A molecular design principle...
