Alberto Minassi
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View article: Mimicking Nature in Reshaping the Triterpene Skeleton: Synthesis of a Class of Unnatural Oleanane Derivatives
Mimicking Nature in Reshaping the Triterpene Skeleton: Synthesis of a Class of Unnatural Oleanane Derivatives Open
The possibility of duplicating the efficiency and selectivity of natural processes under laboratory conditions remains a significant challenge for organic chemists. In this letter, we demonstrated that it is possible to introduce pinpoint …
View article: Optimization of Steroid Photochemistry and Its Application in the Synthesis of 5,6‐Dihydro‐Ophiopogonol A
Optimization of Steroid Photochemistry and Its Application in the Synthesis of 5,6‐Dihydro‐Ophiopogonol A Open
The photoreactivity of steroids represented a hot topic in the middle of the last century and in this project, we “rediscover” it through the exploration of the photochemical behavior of Δ 1 ‐3‐keto‐steroids. In terms of number of products…
View article: The Impact of a Quinone Scaffold on Thermo-TRPs Modulation by Dimethylheptyl Phytocannabinoids
The Impact of a Quinone Scaffold on Thermo-TRPs Modulation by Dimethylheptyl Phytocannabinoids Open
Phytocannabinoids (pCBs) from Cannabis sativa represent an important class of bioactive molecules, potentially useful for the treatment of a wide range of diseases. Their efficacy is due to their ability to interact with multiple targets o…
View article: Stereoselective Shi-type epoxidation with 3-oxo-4,6-<i>O</i>-benzylidene pyranoside catalysts: unveiling the role of carbohydrate skeletons
Stereoselective Shi-type epoxidation with 3-oxo-4,6-<i>O</i>-benzylidene pyranoside catalysts: unveiling the role of carbohydrate skeletons Open
Sugar-derived chiral ketones are capable of reversing stereoselectivity in Shi-type epoxidation.
View article: Trifluoromethyl Ketone Galactose Catalyst for Asymmetric Epoxidation: Experimental and Theoretical Model
Trifluoromethyl Ketone Galactose Catalyst for Asymmetric Epoxidation: Experimental and Theoretical Model Open
Since the introduction of the Shi catalyst, the organocatalytic epoxidation of olefins has become an area of continued research interest. To explore the possibility of enhancing the efficiency and stability of the catalyst, the synthesis o…
View article: Novel Skeletal Rearrangements of the Tigliane Diterpenoid Core
Novel Skeletal Rearrangements of the Tigliane Diterpenoid Core Open
To investigate the role of the secondary 5-hydroxy group in the activity of the anticancer drug tigilanol tiglate (2b) (Stelfonta), oxidation of this epoxytigliane diterpenoid from the Australian rainforest plant Fontainea picros…
View article: Iodine-triphenylphosphine triggers an easy one-pot alpha stereoselective dehydrative glycosylation on hemiacetalic benzylated glycosyl donors
Iodine-triphenylphosphine triggers an easy one-pot alpha stereoselective dehydrative glycosylation on hemiacetalic benzylated glycosyl donors Open
The discovery of new glycosylation reactions is still a major challenge in carbohydrate chemistry. Traditional glycosylation reactions require the preparation of sugar donors with anomeric active or latent leaving groups. Dehydrative glyco…
View article: Recent advances in the development of CB1R selective probes
Recent advances in the development of CB1R selective probes Open
Cannabinoid subtype 1 receptors (CB 1 Rs) are an important class of G protein-coupled receptors (GPCRs) belonging to the endocannabinoid system. CB 1 Rs play a crucial modulatory role in the functioning of other neurotransmitter systems an…
View article: Identification of a Novel Curcumin Derivative Influencing Notch Pathway and DNA Damage as a Potential Therapeutic Agent in T-ALL
Identification of a Novel Curcumin Derivative Influencing Notch Pathway and DNA Damage as a Potential Therapeutic Agent in T-ALL Open
T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematological malignancy considered curable by modern clinical management. Nevertheless, the prognosis for T-ALL high-risk cases or patients with relapsed and refractory disease …
View article: Cannabinol: History, Syntheses, and Biological Profile of the Greatest “Minor” Cannabinoid
Cannabinol: History, Syntheses, and Biological Profile of the Greatest “Minor” Cannabinoid Open
Cannabis (Cannabis sativa L.) is an outstanding source of bioactive natural products, with more than 150 different phytocannabinoids isolated throughout the decades; however, studies of their bioactivity have historically concentrated on t…
View article: Curcumin-based-fluorescent probes targeting ALDH1A3 as a promising tool for glioblastoma precision surgery and early diagnosis
Curcumin-based-fluorescent probes targeting ALDH1A3 as a promising tool for glioblastoma precision surgery and early diagnosis Open
View article: Drug affinity-responsive target stability unveils filamins as biological targets for artemetin, an anti-cancer flavonoid
Drug affinity-responsive target stability unveils filamins as biological targets for artemetin, an anti-cancer flavonoid Open
Artemetin is a valuable 5-hydroxy-3,6,7,3′,4′-pentamethoxyflavone present in many different medicinal plants with very good oral bioavailability and drug-likeness values, owing to numerous bioactivities, such as anti-inflammatory and anti-…
View article: Rotational constriction of curcuminoids impacts 5-lipoxygenase and mPGES-1 inhibition and evokes a lipid mediator class switch in macrophages
Rotational constriction of curcuminoids impacts 5-lipoxygenase and mPGES-1 inhibition and evokes a lipid mediator class switch in macrophages Open
Polypharmacological targeting of lipid mediator networks offers potential for efficient and safe anti-inflammatory therapy. Because of the diversity of its biological targets, curcumin (1a) has been viewed as a privileged structure for bio…
View article: Pyrazole-Curcumin Suppresses Cardiomyocyte Hypertrophy by Disrupting the CDK9/CyclinT1 Complex
Pyrazole-Curcumin Suppresses Cardiomyocyte Hypertrophy by Disrupting the CDK9/CyclinT1 Complex Open
The intrinsic histone acetyltransferase (HAT), p300, has an important role in the development and progression of heart failure. Curcumin (CUR), a natural p300-specific HAT inhibitor, suppresses hypertrophic responses and prevents deteriora…
View article: The synthetic triterpenoids CDDO-TFEA and CDDO-Me, but not CDDO, promote nuclear exclusion of BACH1 impairing its activity
The synthetic triterpenoids CDDO-TFEA and CDDO-Me, but not CDDO, promote nuclear exclusion of BACH1 impairing its activity Open
View article: First thermostable CLIP-tag by rational design applied to an archaeal O-alkyl-guanine-DNA-alkyl-transferase
First thermostable CLIP-tag by rational design applied to an archaeal O-alkyl-guanine-DNA-alkyl-transferase Open
Self-labelling protein tags (SLPs) are resourceful tools that revolutionized sensor imaging, having the versatile ability of being genetically fused with any protein of interest and undergoing activation with alternative probes specificall…
View article: Exploring the Universe of Natural Products: Recent Advances in Synthesis, Isolation and Structural Elucidation
Exploring the Universe of Natural Products: Recent Advances in Synthesis, Isolation and Structural Elucidation Open
Historically, plants have represented an invaluable source of compounds with complex structures and interesting pharmacological profiles [...]
View article: Betulinic Acid Hydroxamate is Neuroprotective and Induces Protein Phosphatase 2A-Dependent HIF-1α Stabilization and Post-transcriptional Dephosphorylation of Prolyl Hydrolase 2
Betulinic Acid Hydroxamate is Neuroprotective and Induces Protein Phosphatase 2A-Dependent HIF-1α Stabilization and Post-transcriptional Dephosphorylation of Prolyl Hydrolase 2 Open
View article: Curcumin-based-fluorescent probes targeting ALDH1A3 as a promising tool for glioblastoma precision surgery and early diagnosis
Curcumin-based-fluorescent probes targeting ALDH1A3 as a promising tool for glioblastoma precision surgery and early diagnosis Open
High Grade Glioma (HGG) is the most aggressive primary brain tumour for which both effective treatments and efficient tools for an early-stage diagnosis are lacking. Herein, we present two curcumin-based fluorescent probes that are able to…
View article: Icilio Guareschi and his amazing “1897 reaction”
Icilio Guareschi and his amazing “1897 reaction” Open
Organic chemistry honors Icilio Guareschi (1847–1918) with three eponymic reactions, the best known ones being the Guareschi synthesis of pyridones and the Guareschi–Lustgarten reaction. A third Guareschi reaction, the so-called “Guareschi…
View article: Biomimetic Approaches to the Synthesis of Natural Disesquiterpenoids: An Update
Biomimetic Approaches to the Synthesis of Natural Disesquiterpenoids: An Update Open
Natural disesquiterpenoids represent a small group of secondary metabolites characterized by complex molecular scaffolds and interesting pharmacological profiles. In the last decade, more than 400 new disesquiterpenoids have been discovere…
View article: The SNAP-<i>tag</i> technology revised: an effective <i>chemo-enzymatic approach</i> by using a universal azide-based substrate
The SNAP-<i>tag</i> technology revised: an effective <i>chemo-enzymatic approach</i> by using a universal azide-based substrate Open
SNAP-tag ® is a powerful technology for the labelling of protein/enzymes by using benzyl-guanine (BG) derivatives as substrates. Although commercially available or ad hoc produced, their synthesis and purification are nec…
View article: Betulinic acid hydroxamate prevents colonic inflammation and fibrosis in murine models of inflammatory bowel disease
Betulinic acid hydroxamate prevents colonic inflammation and fibrosis in murine models of inflammatory bowel disease Open
View article: The Oxidation of Phytocannabinoids to Cannabinoquinoids
The Oxidation of Phytocannabinoids to Cannabinoquinoids Open
Spurred by a growing interest in cannabidiolquinone (CBDQ, HU-313, 2) as a degradation marker and alledged hepatotoxic metabolite of cannabidiol (CBD, 1), we performed a systematic study on the oxidation of CBD (1) to …
View article: The SNAP-<i>tag</i> technology revised: an effective <i>chemo-enzymatic approach</i> by using a universal azide-based substrate
The SNAP-<i>tag</i> technology revised: an effective <i>chemo-enzymatic approach</i> by using a universal azide-based substrate Open
SNAP-tag® is a powerful technology for the labelling of protein/enzymes by using benzyl-guanine (BG) derivatives as substrates. Although commercially available or ad hoc produced, their synthesis and purification are nece…
View article: The dimerization of Δ9-tetrahydrocannabinolic acid A (THCA-A)
The dimerization of Δ9-tetrahydrocannabinolic acid A (THCA-A) Open
View article: Identification of a Strigoterpenoid with Dual Nrf2 and Nf-κB Modulatory Activity
Identification of a Strigoterpenoid with Dual Nrf2 and Nf-κB Modulatory Activity Open
The sesquiterpene-coumarin ether samarcandone provided a suitable framework to replace the apocarotenoid A-C ring system of strigol (1), replicating, after linking to a butenolide moiety, the activity of the natural phytohormone on …
View article: Triterpenoid Hydroxamates as HIF Prolyl Hydrolase Inhibitors
Triterpenoid Hydroxamates as HIF Prolyl Hydrolase Inhibitors Open
Pentacyclic triterpenoid acids (PCTTAs) are pleiotropic agents that target many macromolecular end-points with low to moderate affinity. To explore the biological space associated with PCTTAs, we have investigated the carboxylate-to-hydrox…
View article: Iodine-mediated cyclization of cannabigerol (CBG) expands the cannabinoid biological and chemical space
Iodine-mediated cyclization of cannabigerol (CBG) expands the cannabinoid biological and chemical space Open
View article: Electrophilic Triterpenoid Enones: A Comparative Thiol-Trapping and Bioactivity Study
Electrophilic Triterpenoid Enones: A Comparative Thiol-Trapping and Bioactivity Study Open
Bardoxolone methyl (1) is the quintessential member of triterpenoid cyanoacrylates, an emerging class of bioactive compounds capable of transient covalent binding to thiols. The mechanistic basis for this unusual "pulsed reactivity" profil…