Synthesis, antitumor and antimicrobial evaluation of novel 1,3,4-thiadiazole derivatives bearing disulfide bond

AbstractIn the present study, the synthesis of novel 1,3,4-thiadiazole derivatives bearing disulfide bond are accomplished in good yields with employing a convergent synthetic route, and their in vitro antiproliferative activities were screened against human cancer cell lines A549, Hela, SMMC-7721, and normal cell lines L929 by CCK-8 assay. Meanwhile, all compounds were evaluated for their in vitro antimicrobial activities against Gram-negative bacteriaEscherichia coli and Gram-positive bacteriaStaphylococcus aureus strains. Screening results indicated that some of the tested compounds6a–6h,7a–7h, and8a–8h possessed better antiproliferative activity than positive control 5-fluorouracil. Compounds7f,7h, and8h displayed significant antitumor activities against SMMC-7721 cells with IC50 values 2.37, 3.80, and 2.72  µM, respectively. Compounds6g,7g,7h, and8g showed great antitumor effects against Hela cells with IC50 values 1.29, 2.56, 3.43, and 2.14  µM, respectively. Compounds6e,8a, and8h exhibited highly effective antiproliferative activities against A549 cells with IC50 values 3.43, 2.12, and 3.81  µM, respectively. Most of tested compounds exerted weak cytotoxic effects on normal human cell line L929. Biological evaluation indicated that all the tested compounds possessed antimicrobial activity with certain degrees.

Source: Medicinal Chemistry Research - July 5, 2018 Category: Chemistry Source Type: research