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- Title
The Antiproliferative and Apoptotic Effect of a Novel Synthesized S -Triazine Dipeptide Series, and Toxicity Screening in Zebrafish Embryos.
- Authors
Malebari, Azizah M.; Abd Alhameed, Rakia; Almarhoon, Zainab; Farooq, Muhammad; Wadaan, Mohammad A. M.; Sharma, Anamika; de la Torre, Beatriz G.; Albericio, Fernando; El-Faham, Ayman; Osborn, Helen
- Abstract
Several derivatives containing morpholine/piperidine, anilines, and dipeptides as pending moieties were prepared using s-triazine as a scaffold. These compounds were evaluated for their anticancer activity against two human breast cancer cell lines (MCF-7 and MDA-MB-231), a colon cancer cell line (HCT-116), and a non-tumorigenic cell line (HEK 293). Tamoxifen was used as a reference. Animal toxicity tests were carried out in zebrafish embryos. Most of these compounds showed a higher activity against breast cancer than colon cancer. Compound 3a—which contains morpholine, aniline, and glycylglycinate methyl ester—showed a high level of cytotoxicity against MCF-7 cells with IC50 values of less than 1 µM. This compound showed a much lower level of toxicity against the non-tumorigenic HEK-293 cell line, and in the in vivo studies using zebrafish embryos. Furthermore, it induced cell cycle arrest at the G2/M phase, and apoptosis in MCF-7 cells. On the basis of our results, 3a emerges as a potential candidate for further development as a therapeutic drug to treat hormone receptor-positive breast cancer.
- Subjects
ZEBRA danio embryos; BRACHYDANIO; EMBRYOS; CELL cycle; COLON cancer; CELL lines; ZEBRA danio; TRIAZINE derivatives
- Publication
Molecules, 2021, Vol 26, Issue 4, p1170
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules26041170