دورية أكاديمية
Design, Synthesis, Molecular Modeling and Antitumor Evaluation of Novel Indolyl-Pyrimidine Derivatives with EGFR Inhibitory Activity.
العنوان: | Design, Synthesis, Molecular Modeling and Antitumor Evaluation of Novel Indolyl-Pyrimidine Derivatives with EGFR Inhibitory Activity. |
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المؤلفون: | Ahmed NM; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ein-Helwan, Helwan, Cairo 11795, Egypt., Youns MM; Biochemistry Department, Faculty of Pharmacy, Helwan University, Ein-Helwan, Helwan, Cairo 11795, Egypt.; Oman College of Health Sciences, Muscat 123, Oman., Soltan MK; Oman College of Health Sciences, Muscat 123, Oman.; Medicinal Chemistry Department, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt., Said AM; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ein-Helwan, Helwan, Cairo 11795, Egypt.; Department of Chemistry, University at Buffalo, The State University of New York, Buffalo, NY 14260, USA. |
المصدر: | Molecules (Basel, Switzerland) [Molecules] 2021 Mar 25; Vol. 26 (7). Date of Electronic Publication: 2021 Mar 25. |
نوع المنشور: | Journal Article |
اللغة: | English |
بيانات الدورية: | Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE |
أسماء مطبوعة: | Original Publication: Basel, Switzerland : MDPI, c1995- |
مواضيع طبية MeSH: | Antineoplastic Agents*/chemical synthesis , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/pharmacology , Models, Molecular* , Neoplasm Proteins*/antagonists & inhibitors , Neoplasm Proteins*/metabolism , Pyrimidines*/chemical synthesis , Pyrimidines*/chemistry , Pyrimidines*/pharmacology, Neoplasms/*drug therapy, Animals ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/metabolism ; HCT116 Cells ; Hep G2 Cells ; Humans ; MCF-7 Cells ; Mice ; Neoplasms/metabolism ; Neoplasms/pathology ; Xenograft Model Antitumor Assays |
مستخلص: | Scaffolds hybridization is a well-known drug design strategy for antitumor agents. Herein, series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in vivo for their antitumor activity. The in vitro antiproliferative activity of all compounds was obtained against MCF-7, HepG2, and HCT-116 cancer cell lines, as well as against WI38 normal cells using the resazurin assay. Compounds 1 - 4 showed broad spectrum cytotoxic activity against all these cancer cell lines compared to normal cells. Compound 4g showed potent antiproliferative activity against these cell lines (IC |
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فهرسة مساهمة: | Keywords: EGFR; cancer; drug design; indole; molecular modeling; pyrimidine |
المشرفين على المادة: | 0 (Antineoplastic Agents) 0 (Neoplasm Proteins) 0 (Pyrimidines) EC 2.7.10.1 (EGFR protein, human) EC 2.7.10.1 (ErbB Receptors) |
تواريخ الأحداث: | Date Created: 20210403 Date Completed: 20210512 Latest Revision: 20210512 |
رمز التحديث: | 20240628 |
مُعرف محوري في PubMed: | PMC8037142 |
DOI: | 10.3390/molecules26071838 |
PMID: | 33805918 |
قاعدة البيانات: | MEDLINE |
تدمد: | 1420-3049 |
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DOI: | 10.3390/molecules26071838 |