New Structural Features of Isatin Dihydrothiazole Hybrids for Selective Carbonic Anhydrase Inhibitors.

Chemotherapeutic agents have remained the first-line treatment option for advanced-stage cancers when surgery or radiation therapy is not viable. Human carbonic anhydrase (hCA) isoforms IX and XII have been validated as anticancer targets. In particular, hCA IX is overexpressed in several solid tumor cells.

Exploring the 1-(4-Nitrophenyl)-3-arylprop-2-en-1-one Scaffold for the Selective Inhibition of Monoamine Oxidase B.

A small library of 1-(4-nitrophenyl)-3-arylprop-2-en-1-one derivatives was synthesized to identify new human monoamine oxidase B selective inhibitors. Their inhibitory activity toward MAO-A and MAO-B isoforms was evaluated to determine their potency and selectivity. All newly synthesized compounds were nanomolar inhibitors of the B isoform with IC concentrations ranging from 120 to 2.

Privileged Scaffold Hybridization in the Design of Carbonic Anhydrase Inhibitors.

Human Carbonic Anhydrases (hCA) are enzymes that contribute to cancer's development and progression. Isoforms IX and XII have been identified as potential anticancer targets, and, more specifically, hCA IX is overexpressed in hypoxic tumor cells, where it plays an important role in reprogramming the metabolism. With the aim to find new inhibitors towards IX and XII isoforms, the hybridization of the privileged scaffolds isatin, dihydrothiazole, and benzenesulfonamide was investigated in order to explore how it may affect the activity and selectivity of the hCA isoforms.

Tracking Response and Resistance in Acute Myeloid Leukemia through Single-Cell DNA Sequencing Helps Uncover New Therapeutic Targets.

Acute myeloid leukemia (AML) is an aggressive hematologic neoplasia with a complex polyclonal architecture. Among driver lesions, those involving the gene represent the most frequent mutations identified at diagnosis. The development of tyrosine kinase inhibitors (TKIs) has improved the clinical outcomes of -mutated patients (Pt).

Antibacterial Activity of Amidodithiophosphonato Nickel(II) Complexes: An Experimental and Theoretical Approach.

The reactions of 2,4-bis(4-methoxyphenyl)-1,3-dithio-2,4-diphosphetane-2,4-disulfide (Lawesson's Reagent, LR) with benzylamine (BzNH) and 4-phenylbutylamine (PhBuNH) yield benzylammonium -(4-methoxyphenyl)--benzyl-amidodithiophosphonate (BzNH)(BzNH-adtp) and 4-phenylbutylammonium -(4-methoxyphenyl)--(4-phenylbutyl)-amidodithiophosphonate (PhBuNH)(PhBuNH-adtp). The relevant nickel complexes [Ni(BzNH-adtp)] and [Ni(PhBuNH-adtp)] and the corresponding hydrolysed derivatives (BzNH)[Ni(dtp)] and (PhBuNH)[Ni(dtp)] were prepared and fully characterized. The antimicrobial activity of the aforementioned amidodithiophosphonates against a set of Gram-positive and Gram-negative pathogen bacteria was evaluated, and [Ni(BzNH-adtp)] and [Ni(PhBuNH-adtp)] showed antiproliferative activity towards and strains.