Synthesis, Characterization, In Vitro Anticancer Evaluation, ADMET Properties, and Molecular Docking of Novel 5-Sulfanyl Substituted (Thiazol-4-yl)-Phosphonium Salts.

Seven TPP+ new 5-sulfanyl substituted (thiazol-4-yl) phosphonium salts functionalized with different substituents were designed, synthesized, and studied against the NCI-60 human cancer cell lines. Compounds 1-4 show the total average parameters GI=0.7-2.

Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors.

A series of benzenesulfonamides incorporating pyrazole- and pyridazinecarboxamides decorated with several bulky moieties has been obtained by original procedures. The new derivatives were investigated for the inhibition of four physiologically crucial human carbonic anhydrase (hCA, EC 4.2.

New Sulfanilamide Derivatives Incorporating Heterocyclic Carboxamide Moieties as Carbonic Anhydrase Inhibitors.

Carbonic Anhydrases (CAs) are ubiquitous metalloenzymes involved in several disease conditions. There are 15 human CA (hCA) isoforms and their high homology represents a challenge for the discovery of potential drugs devoid of off-target side effects. For this reason, many synthetic and pharmacologic research efforts are underway to achieve the full pharmacological potential of CA modulators of activity.

Rapid synthetic approaches to libraries of diversified 1,2-dihydrochromeno[2,3-c]pyrrole-3,9-diones and 3-(2-hydroxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H)-ones.

An efficient and practical synthetic procedure for libraries of diversified 1,2-dihydrochromeno[2,3-c]pyrrole-3,9-diones using a multicomponent process is presented. A convenient synthetic procedure for obtaining functionalized 3-(2-hydroxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H)-ones via ring-opening strategy has also been developed. This protocol was found to be compatible with a wide range of substituents and paves the way for the practical synthesis of title compounds with a broad range of substituents under mild condition.