دورية أكاديمية
Design, synthesis and molecular docking of novel diarylcyclohexenone and diarylindazole derivatives as tubulin polymerization inhibitors.
| العنوان: | Design, synthesis and molecular docking of novel diarylcyclohexenone and diarylindazole derivatives as tubulin polymerization inhibitors. |
|---|---|
| المؤلفون: | Ahmed RI; a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Nahda University in Beni Suef , Kornish Al Nile , Beni Suef , Egypt., Osman EE; b Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Cairo University , Cairo , Egypt., Awadallah FM; b Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Cairo University , Cairo , Egypt., El-Moghazy SM; b Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Cairo University , Cairo , Egypt. |
| المصدر: | Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2017 Dec; Vol. 32 (1), pp. 176-188. Date of Electronic Publication: 2016 Oct 24. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Taylor & Francis Country of Publication: England NLM ID: 101150203 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1475-6374 (Electronic) Linking ISSN: 14756366 NLM ISO Abbreviation: J Enzyme Inhib Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Basingstoke, UK : Taylor & Francis, c2002- |
| مواضيع طبية MeSH: | Molecular Docking Simulation*, Cyclohexenes/*chemical synthesis , Cyclohexenes/*pharmacology , Indazoles/*chemical synthesis , Indazoles/*pharmacology , Tubulin Modulators/*chemical synthesis , Tubulin Modulators/*pharmacology, Carbon-13 Magnetic Resonance Spectroscopy ; Humans ; Polymerization ; Proton Magnetic Resonance Spectroscopy ; Spectrometry, Mass, Electrospray Ionization |
| مستخلص: | New target compounds were designed as inhibitors of tubulin polymerization relying on using two types of ring B models (cyclohexenone and indazole) to replace the central ring in colchicine. Different functional groups (R 1 ) were attached to manipulate their physicochemical properties and/or their biological activity. The designed compounds were assessed for their antitumor activity on HCT-116 and MCF-7 cancer cell lines. Compounds 4b, 5e and 5f exhibited comparable or higher potency than colchicine against colon HCT-116 and MCF-7 tumor cells. The mechanism of the antitumor activity was investigated through evaluating the tubulin inhibition potential of the active compounds. Compounds 4b, 5e and 5f showed percentage inhibition of tubulin in both cell line homogenates ranging from 79.72% to 89.31%. Cell cycle analysis of compounds 4b, 5e and 5f revealed cell cycle arrest at G |
| References: | Top Curr Chem. 2009;286:279-328. (PMID: 23563616) Bioorg Med Chem Lett. 2007 Nov 1;17(21):5897-901. (PMID: 17827004) Molecules. 2011 Aug 08;16(8):6684-700. (PMID: 25134772) Eur J Med Chem. 2013 Jan;59:120-31. (PMID: 23229055) Nature. 2004 Mar 11;428(6979):198-202. (PMID: 15014504) Bioorg Med Chem. 2011 Apr 1;19(7):2306-25. (PMID: 21397510) Chem Biol Drug Des. 2015 Oct;86(4):731-45. (PMID: 25711282) Bioorg Med Chem. 2009 Sep 15;17(18):6780-5. (PMID: 19683930) J Med Chem. 2009 Mar 26;52(6):1701-11. (PMID: 19243174) Bioorg Med Chem Lett. 2001 Sep 3;11(17):2341-3. (PMID: 11527727) J Med Chem. 2003 Dec 4;46(25):5437-44. (PMID: 14640552) J Appl Toxicol. 2013 Jun;33(6):426-33. (PMID: 22081495) Clin Cancer Res. 2011 Aug 1;17(15):5152-60. (PMID: 21690571) FEBS Lett. 1983 Sep 5;161(1):55-9. (PMID: 6884527) J Med Chem. 2002 Apr 11;45(8):1697-711. (PMID: 11931625) Pharm Res. 2012 Nov;29(11):2943-71. (PMID: 22814904) |
| فهرسة مساهمة: | Keywords: Antimitotic agent; cell cycle; colchicine; docking; tubulin |
| المشرفين على المادة: | 0 (Cyclohexenes) 0 (Indazoles) 0 (Tubulin Modulators) |
| تواريخ الأحداث: | Date Created: 20161025 Date Completed: 20170221 Latest Revision: 20181113 |
| رمز التحديث: | 20231215 |
| مُعرف محوري في PubMed: | PMC6009925 |
| DOI: | 10.1080/14756366.2016.1244532 |
| PMID: | 27771966 |
| قاعدة البيانات: | MEDLINE |
PDF full text from Publisher 
Full Text Finder | تدمد: | 1475-6374 |
|---|---|
| DOI: | 10.1080/14756366.2016.1244532 |