دورية أكاديمية
أعرض في EDS

Synthesis and Biological Activity Screening of Newly Synthesized Trimethoxyphenyl-Based Analogues as Potential Anticancer Agents.

التفاصيل البيبلوغرافية
العنوان: Synthesis and Biological Activity Screening of Newly Synthesized Trimethoxyphenyl-Based Analogues as Potential Anticancer Agents.
المؤلفون: Al-Warhi T; Department of Chemistry, College of Science, Princess Nourah Bint Abdulrahman University, Riyadh 11671, Saudi Arabia., Abualnaja M; Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, Makkah Al Mukarrama 24381, Saudi Arabia., Abu Ali OA; Department of Chemistry, College of Science, Taif University, Taif 21944, Saudi Arabia., Althobaiti F; Department of Biotechnology, Faculty of Sciences, Taif University, Taif 21944, Saudi Arabia., Alharthi F; Department of Biology, College of Science, Taif University, Taif 21944, Saudi Arabia., Elsaid FG; Biology Department, Science College, King Khalid University, Abha 61421, Saudi Arabia.; Zoology Department, Faculty of Science, Mansoura University, Mansoura 35516, Egypt., Shati AA; Biology Department, Science College, King Khalid University, Abha 61421, Saudi Arabia., Fayad E; Department of Biotechnology, Faculty of Sciences, Taif University, Taif 21944, Saudi Arabia., Elghareeb D; Department of Biology, Jumum College University, Umm Al-Qura University, Makkah 21955, Saudi Arabia.; Agriculture Genetic Engineering Research Institute (AGERI), Agriculture Research Centre, Cairo 12619, Egypt., Abu Almaaty AH; Zoology Department, Faculty of Science, Port Said University, Port Said 42526, Egypt., Zaki I; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said 42526, Egypt.
المصدر: Molecules (Basel, Switzerland) [Molecules] 2022 Jul 20; Vol. 27 (14). Date of Electronic Publication: 2022 Jul 20.
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*/chemistry , Apoptosis*, Cell Line, Tumor ; Cell Proliferation ; Drug Screening Assays, Antitumor ; Molecular Structure ; Structure-Activity Relationship ; Tubulin/metabolism ; Tubulin Modulators/pharmacology
مستخلص: A group of novel trimethoxyphenyl (TMP)-based analogues were synthesized by varying the azalactone ring of 2-(3,4-dimethoxyphenyl)-4-(3,4,5-trimethoxybenzylidene)oxazolone 1 and characterized using NMR spectral data as well as elemental microanalyses. All synthesized compounds were screened for their cytotoxic activity utilizing the hepatocellular carcinoma (HepG2) cell line. Compounds 9 , 10 and 11 exhibited good cytotoxic potency with IC 50 values ranging from 1.38 to 3.21 μM compared to podophyllotoxin (podo) as a reference compound. In addition, compounds 9 , 10 and 11 exhibited potent inhibition of β-tubulin polymerization. DNA flow cytometry analysis of compound 9 shows cell cycle disturbance at the G2/M phase and a significant increase in Annexin-V-positive cells compared with the untreated control. Compound 9 was further studied regarding its apoptotic potential in HepG2 cells; it decreased the level of MMP and Bcl-2 as well as boosted the level of p53 and Bax compared with the control HepG2 cells.
References: Angew Chem Int Ed Engl. 2021 Jun 7;60(24):13331-13342. (PMID: 33951246)
Future Oncol. 2021 Oct;17(30):4011-4025. (PMID: 34337973)
Expert Rev Anticancer Ther. 2021 Nov;21(11):1207-1210. (PMID: 34493147)
Invest New Drugs. 2021 Oct;39(5):1222-1231. (PMID: 33788074)
Curr Biol. 2021 May 24;31(10):R506-R511. (PMID: 34033781)
ACS Omega. 2021 Sep 15;6(38):25002-25009. (PMID: 34604680)
Int J Mol Sci. 2022 Apr 04;23(7):. (PMID: 35409361)
Bioorg Med Chem Lett. 2016 Jul 1;26(13):3001-3005. (PMID: 27212068)
Pharmaceutics. 2021 Feb 25;13(3):. (PMID: 33668877)
Bioorg Chem. 2021 Jul;112:104904. (PMID: 33933802)
Nat Rev Mol Cell Biol. 2022 Aug;23(8):541-558. (PMID: 35383336)
J Med Chem. 2013 Apr 25;56(8):3318-29. (PMID: 23547728)
Mol Oncol. 2015 Feb;9(2):488-502. (PMID: 25458053)
Pharmaceuticals (Basel). 2022 May 28;15(6):. (PMID: 35745599)
Eur J Med Chem. 2010 Sep;45(9):3960-9. (PMID: 20573424)
Eur J Pharmacol. 2020 Jun 15;877:173093. (PMID: 32234525)
Curr Biol. 2020 Jun 8;30(11):2184-2190.e5. (PMID: 32386526)
Curr Opin Struct Biol. 2021 Feb;66:193-198. (PMID: 33296732)
Anticancer Agents Med Chem. 2022;22(11):2048-2062. (PMID: 34825878)
J Enzyme Inhib Med Chem. 2022 Dec;37(1):9-38. (PMID: 34894980)
J Med Chem. 2022 Mar 24;65(6):4578-4589. (PMID: 35238566)
Arch Pharm (Weinheim). 2014 Sep;347(9):658-67. (PMID: 24996189)
Basic Clin Pharmacol Toxicol. 2022 Jan;130 Suppl 1:60-74. (PMID: 34481421)
Future Med Chem. 2021 May;13(9):839-858. (PMID: 33821673)
Cells. 2019 Apr 12;8(4):. (PMID: 31013740)
Front Pharmacol. 2021 Jan 20;11:553404. (PMID: 33628166)
Nat Rev Cancer. 2022 Jun;22(6):323-339. (PMID: 35264777)
Cell J. 2021 Jan;22(4):532-541. (PMID: 32347047)
معلومات مُعتمدة: PNURSP2022R25 Princess Nourah bint Abdulrahman University Researchers Supporting Project number (PNURSP2022R25), Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia
فهرسة مساهمة: Keywords: apoptosis; cell cycle analysis; cytotoxicity; diamide; imidazolone; oxazolone; triazinone; tubulin
المشرفين على المادة: 0 (Antineoplastic Agents)
0 (Tubulin)
0 (Tubulin Modulators)
تواريخ الأحداث: Date Created: 20220727 Date Completed: 20220728 Latest Revision: 20220731
رمز التحديث: 20240829
مُعرف محوري في PubMed: PMC9322052
DOI: 10.3390/molecules27144621
PMID: 35889493
قاعدة البيانات: MEDLINE
الوصف
تدمد:1420-3049
DOI:10.3390/molecules27144621