Design and synthesis of 21-alkynylaryl pregnenolone derivatives and evaluation of their anticancer activity

A simple open source bioinformatic methodology for initial exploration of GPCR ligands’ agonistic/antagonistic properties

“…In addition to the above compounds, we have tested a series of pregnenolone analogs, with reported antiproliferative activity in different cancer cell lines. 34 As shown in In order to verify our prediction, we have experimentally tested whether these compounds can antagonize 5-oxo-ETE action on cAMP production, like testosterone 38 OXER1-G αi interaction results in an inhibition of cAMP. [36][37][38] This is experimentally tested by stimulating cAMP production in cells by forskolin and detecting the cAMP inhibition after incubation of cells with the corresponding ligands.…”

Synthesis and Evaluation of New Potential Benzo[a]phenoxazinium Photosensitizers for Anticancer Photodynamic Therapy

“…Pregnenolone, known as a precursor to most hormones, had been explored as carrier of anticancer drugs [ 25 ]. In addition, several types of pregnenolone derivatives were reported to have anticancer activity by our and other groups [ 26 , 27 , 28 ]. PS5 was synthesized as the first benzo[ a ]phenoxazinium dimer to determine the superimposed effect of the benzo[ a ]phenoxazinium core on anticancer PDT efficacy.…”

Novel porphyrin–Schiff base conjugates: synthesis, characterization and in vitro photodynamic activities

“…For example, pregnenolone derivatives containing heterocyclic moieties were found to exhibit anticancer activity. 23,24 In addition, suitable photosensitizer candidates were obtained by attaching various substituents to the peripheral positions of the porphyrin core.…”