دورية أكاديمية
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Novel indolyl 1,2,4-triazole derivatives as potential anti-proliferative agents: in silico studies, synthesis, and biological evaluation.

التفاصيل البيبلوغرافية
العنوان: Novel indolyl 1,2,4-triazole derivatives as potential anti-proliferative agents: in silico studies, synthesis, and biological evaluation.
المؤلفون: Ghobish SA; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Misr International University Cairo Egypt nahla.farag@miuegypt.edu.eg doaa.boshra@miuegypt.edu.eg., Mohamed KO; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University Cairo Egypt.; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Sinai University (Arish branch) El Arish Egypt., Farag N; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Misr International University Cairo Egypt nahla.farag@miuegypt.edu.eg doaa.boshra@miuegypt.edu.eg., Farag DB; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Misr International University Cairo Egypt nahla.farag@miuegypt.edu.eg doaa.boshra@miuegypt.edu.eg.
المصدر: RSC medicinal chemistry [RSC Med Chem] 2023 Nov 24; Vol. 15 (1), pp. 293-308. Date of Electronic Publication: 2023 Nov 24 (Print Publication: 2024).
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Royal Society of Chemistry Country of Publication: England NLM ID: 101759460 Publication Model: eCollection Cited Medium: Internet ISSN: 2632-8682 (Electronic) Linking ISSN: 26328682 NLM ISO Abbreviation: RSC Med Chem Subsets: PubMed not MEDLINE
أسماء مطبوعة: Original Publication: Cambridge : Royal Society of Chemistry, [2020]-
مستخلص: A new series of indolyl 1,2,4-triazole scaffolds was designed, synthesised, and biologically evaluated for their inhibitory activity against both CDK4 and CDK6. The results ranged from 0.049 μM to 3.031 μM on CDK4 and from 0.075 μM to 1.11 μM on CDK6 when compared to staurosporine, with IC 50 values of 1.027 and 0.402 μM, respectively. Moreover, all compounds were tested for their cytotoxicity against two breast cancer cell lines, MCF-7 and MDA-MB-231. All of the synthesised compounds showed promising anti-proliferative activity, with two compounds Vf (IC 50 = 2.91 and 1.914 μM, respectively) and Vg (IC 50 = 0.891 and 3.479 μM, respectively) having potent cytotoxic activity in comparison to the reference staurosporine (IC 50 = 3.144 and 4.385 μM, respectively). Vf and Vg were also found to significantly induce apoptosis to 45.33% and 37.26% (control = 1.91%) where Vf arrested the cell cycle at the S phase while Vg arrested the cycle at the G 0 /G 1 phase. The binding mode and interactions of all compounds were studied and found to mimic those of the FDA approved CDK4/6 inhibitor palbociclib that was used as a reference throughout the study.
Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(This journal is © The Royal Society of Chemistry.)
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تواريخ الأحداث: Date Created: 20240129 Latest Revision: 20240130
رمز التحديث: 20240130
مُعرف محوري في PubMed: PMC10809324
DOI: 10.1039/d3md00524k
PMID: 38283222
قاعدة البيانات: MEDLINE
الوصف
تدمد:2632-8682
DOI:10.1039/d3md00524k