Baharloui Maryam, Mirshokraee Sayed Ahmmad, Monfared Azam, Houshdar Tehrani Mohammad Hassan
Department of Chemistry, Faculty of Basic Sciences, Payam Noor University, Tehran, Iran.
Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Iran J Pharm Res. 2019 Summer;18(3):1299-1308. doi: 10.22037/ijpr.2019.111722.13320.
Cancer disease is a great concern in the worldwide public health and current treatments do not give satisfactory results, so, developing novel therapeutic agents to combat cancer is highly demanded. Nowadays, anticancer peptides (ACPs) are becoming promising anticancer drug candidates. This is due to several advantages inherited in peptide molecules, such as being usually with small size, high activity, low immunogenicity, good biocompatibility, diversity of sequence, and more modification sites for functionalization. To get benefit of these merits, in this work, we synthesized a new series of triazole- based analogues with peptide scaffold by employing click chemistry and evaluated their anticancer activities against breast, colon cancer cell lines as well as fibroblast cells using MTT assay. Our results suggest that peptide scaffolds containing 1-1, 2, 3-triazole ring group are toxic against colon and breast cancer cells viability, and this effect was more pronounced on MDA-MB-231 cells compared with MCF-7 breast cells. As a conclusion, these designed peptide analogues may be good and safe candidates as future anticancer agents.
癌症是全球公共卫生领域极为关注的问题，目前的治疗方法并未取得令人满意的效果，因此，迫切需要开发新型抗癌药物。如今，抗癌肽（ACPs）正成为有前景的抗癌药物候选物。这是由于肽分子具有若干固有优势，例如通常尺寸小、活性高、免疫原性低、生物相容性好、序列多样性以及更多用于功能化的修饰位点。为了利用这些优点，在本研究中，我们通过点击化学合成了一系列以肽为骨架的新型三唑基类似物，并使用MTT法评估了它们对乳腺癌、结肠癌细胞系以及成纤维细胞的抗癌活性。我们的结果表明，含有1,2,3 - 三唑环基团的肽骨架对结肠和乳腺癌细胞的活力具有毒性，与MCF - 7乳腺癌细胞相比，这种作用在MDA - MB - 231细胞上更为明显。总之，这些设计的肽类似物可能是未来抗癌药物的良好且安全的候选物。
