The Antiproliferative and Apoptotic Effect of a Novel Synthesized -Triazine Dipeptide Series, and Toxicity Screening in Zebrafish Embryos

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2021 Mar 6

PMID 33671801

Citations 4

Authors

Azizah M Malebari

Rakia Abd Alhameed

Zainab Almarhoon

Muhammad Farooq

Mohammad A M Wadaan

Anamika Sharma

Beatriz G de la Torre

Fernando Albericio

Ayman El-Faham

Affiliations

Soon will be listed here.

Abstract

Several derivatives containing morpholine/piperidine, anilines, and dipeptides as pending moieties were prepared using -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 -which contains morpholine, aniline, and glycylglycinate methyl ester-showed a high level of cytotoxicity against MCF-7 cells with IC 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, emerges as a potential candidate for further development as a therapeutic drug to treat hormone receptor-positive breast cancer.

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