"Angular" Spirocyclic Azetidines: Synthesis, Characterization, and Evaluation in Drug Discovery.

The previously neglected "angular" spirocyclic azetidines have been synthesized, characterized, and validated in drug discovery. We have shown that these compounds could act as bioisosteres for common saturated six-membered heterocycles. Their incorporation into the structure of the anticancer drug Sonidegib (instead of morpholine), and Danofloxacine (instead of piperazine) provided novel patent-free analogs with similar physicochemical properties and high activity.

CF-Cyclobutanes: Synthesis, Properties, and Evaluation as a Unique -Butyl Group Analogue.

Isosteric replacement of functional groups is an emerging strategy for optimizing bioactive molecules in drug discovery. -Butyl group is a particularly important moiety, yet its isosteric replacement with 1-trifluoromethyl-cyclobutyl group has been rather neglected. To enable the advance of this molecular fragment in drug discovery programs, we report the synthesis of over 30 small-molecule building blocks featuring the trifluoromethyl-cyclobutyl fragment, achieved by reacting sulfur tetrafluoride with cyclobutylcarboxylic acids on a gram-to-multigram scale.

1,2-Disubstituted bicyclo[2.1.1]hexanes as saturated bioisosteres of -substituted benzene.

Bicyclo[2.1.1]hexanes have been synthesized, characterized, and biologically validated as saturated bioisosteres of the -substituted benzene ring.

2-Oxabicyclo[2.1.1]hexanes as saturated bioisosteres of the ortho-substituted phenyl ring.

The ortho-substituted phenyl ring is a basic structural element in chemistry. It is found in more than three hundred drugs and agrochemicals. During the past decade, scientists have tried to replace the phenyl ring in bioactive compounds with saturated bioisosteres to obtain novel patentable structures.

ANTIPROLIFERATIVE ACTIVITIES Of EXTRACTS FROM MYCELIAL BIOMASS OF SOME MEDICINAL BASIDIOMYCETES IN HUMAN COLON CANCER CELLS COLO 205.

Background: The anticancer effects of phytohormones of cytokinin nature are similar to those of medicinal mushrooms, which are able to synthesize cytokinins in large amounts.

Aim: To determine the antiproliferative effect of crude extracts and cytokinin fractions from the mycelial biomass of seven fungi species on colon cancer cells in vitro.

Materials And Methods: Cytokinin content in mycelial biomass of Ganoderma lucidum, Lentinula edodes, Trametes versicolor, Pleurotus ostreatus, Morchella esculenta, Hericium coralloides, and Fomitopsis officinalis was determined by high performance liquid chromatography mass spectrometry.