Literature DB >> 25180925

Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents.

Li-Ying Ma1, Lu-Ping Pang1, Bo Wang1, Miao Zhang1, Biao Hu1, Deng-Qi Xue1, Kun-Peng Shao1, Bao-Le Zhang1, Ying Liu1, En Zhang1, Hong-Min Liu2.   

Abstract

A series of novel 1,2,3-triazole-pyrimidine hybrids were designed, synthesized and evaluated for their anticancer activity against four selected cancer cell lines (MGC-803, EC-109, MCF-7 and B16-F10). Most of the synthesized compounds exhibited moderate to good activity against all the cancer cell lines selected. Compound 17 showed the most excellent anticancer activity with single-digit micromolar IC50 values ranging from 1.42 to 6.52 μM. Further mechanism studies revealed that compound 17 could obviously inhibit the proliferation of EC-109 cancer cells by inducing apoptosis and arresting the cell cycle at G2/M phase.
Copyright © 2014. Published by Elsevier Masson SAS.

Entities:  

Keywords:  Anticancer; Apoptosis; Cell cycle arrest; Pyrimidine; Triazole

Mesh：

Substances：

Year:  2014        PMID： 25180925     DOI： 10.1016/j.ejmech.2014.08.010

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  8 in total

1.  The Design and Synthesis of a New Series of 1,2,3-Triazole-Cored Structures Tethering Aryl Urea and Their Highly Selective Cytotoxicity toward HepG2.

Authors:  Sittisak Oekchuae; Jitnapa Sirirak; Purin Charoensuksai; Pawaris Wongprayoon; Natthaya Chuaypen; Jutatip Boonsombat; Somsak Ruchirawat; Pisit Tangkijvanich; Apichart Suksamrarn; Panupun Limpachayaporn
Journal:  Pharmaceuticals (Basel)       Date:  2022-04-20

2.  Discovery of 5,6-diaryl-1,2,4-triazines hybrids as potential apoptosis inducers.

Authors:  Dong-Jun Fu; Jian Song; Yu-Hui Hou; Ruo-Han Zhao; Jia-Huan Li; Ruo-Wang Mao; Jia-Jia Yang; Ping Li; Xiao-Lin Zi; Zhong-Hua Li; Qing-Qing Zhang; Fei-Yan Wang; Sai-Yang Zhang; Yan-Bing Zhang; Hong-Min Liu
Journal:  Eur J Med Chem       Date:  2017-07-08       Impact factor: 6.514

3.  Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition.

Authors:  Zafer Sahin; Sevde Nur Biltekin; Leyla Yurttas; Barkin Berk; Yağmur Özhan; Hande Sipahi; Zhan-Guo Gao; Kenneth A Jacobson; Şeref Demirayak
Journal:  Eur J Med Chem       Date:  2020-12-31       Impact factor: 6.514

4.  Synthesis and biological evaluation of 4-(1H-1,2,4-triazol-1-yl)benzoic acid hybrids as anticancer agents.

Authors:  Hatem A Abuelizz; Hanem M Awad; Mohamed Marzouk; Fahd A Nasr; Ali S Alqahtani; Ahmed H Bakheit; Ahmed M Naglah; Rashad Al-Salahi
Journal:  RSC Adv       Date:  2019-06-17       Impact factor: 4.036

Review 5.  Triazole analogues as potential pharmacological agents: a brief review.

Authors:  Sachin Kumar; Sukhbir Lal Khokra; Akash Yadav
Journal:  Futur J Pharm Sci       Date:  2021-05-25

6.  Theoretical calculations of molecular descriptors for anticancer activities of 1, 2, 3-triazole-pyrimidine derivatives against gastric cancer cell line (MGC-803): DFT, QSAR and docking approaches.

Authors:  Rhoda Oyeladun Oyewole; Abel Kolawole Oyebamiji; Banjo Semire
Journal:  Heliyon       Date:  2020-05-21

7.  Design, Synthesis and Anticancer Screening of Novel Benzothiazole-Piperazine-1,2,3-Triazole Hybrids.

Authors:  Mohamed R Aouad; Moataz A Soliman; Muath O Alharbi; Sanaa K Bardaweel; Pramod K Sahu; Adeeb A Ali; Mouslim Messali; Nadjet Rezki; Yaseen A Al-Soud
Journal:  Molecules       Date:  2018-10-27       Impact factor: 4.411

8.  Click chemistry based synthesis, cytotoxic activity and molecular docking of novel triazole-thienopyrimidine hybrid glycosides targeting EGFR.

Authors:  Reham R Khattab; Asma K Alshamari; Allam A Hassan; Hussein H Elganzory; Wael A El-Sayed; Hanem M Awad; Eman S Nossier; Nasser A Hassan
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051
  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.