Literature DB >> 25554922

Novel pyrazole-5-carboxamide and pyrazole-pyrimidine derivatives: synthesis and anticancer activity.

Jing Bo Shi1, Wen Jian Tang2, Xing Bao Qi2, Rong Li2, Xin Hua Liu3.   

Abstract

A series of novel pyrazole-5-carboxamide and pyrazole-pyrimidine derivatives were designed and synthesized. All compounds have been screened for their antiproliferative activity against MGC-803, SGC-7901 and Bcap-37 cell lines in vitro. The results revealed that compounds 8a, 8c and 8e exhibited strong inhibitory activity against MGC-803 cell line. The flow cytometric analysis result showed that compound 8e could inhibit MGC-803 proliferation. Some title compounds were tested against telomerase, and compound 8e showed the most potent inhibitory activity with IC50 value at 1.02 ± 0.08 μM. The docking simulation of compound 8e was performed to get the probable binding model, among them, LYS 189, LYS 372, LYS 249 and ASP 254 may be the key residues for the telomerase activity.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Anticancer activity; Pyrazole-5-carboxamide; Synthesis; Telomerase

Mesh：

Substances：

Year:  2014        PMID： 25554922     DOI： 10.1016/j.ejmech.2014.12.013

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


  7 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

Review 2.  Chemical Compounds of Berry-Derived Polyphenols and Their Effects on Gut Microbiota, Inflammation, and Cancer.

Authors:  Abdelhakim Bouyahya; Nasreddine El Omari; Naoufal El Hachlafi; Meryem El Jemly; Maryam Hakkour; Abdelaali Balahbib; Naoual El Menyiy; Saad Bakrim; Hanae Naceiri Mrabti; Aya Khouchlaa; Mohamad Fawzi Mahomoodally; Michelina Catauro; Domenico Montesano; Gokhan Zengin
Journal:  Molecules       Date:  2022-05-20       Impact factor: 4.927

3.  Design and synthesis of novel (Z)-5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)-3-((1-substituted phenyl-1H-1,2,3-triazol-4-yl)methyl)thiazolidine-2,4-diones: a potential cytotoxic scaffolds and their molecular modeling studies.

Authors:  N J P Subhashini; Kolluri Prashanth Kumar; Edigi Praveen Kumar; Putta Shravani; Surya Sathyanarayana Singh; Tamalapakula Vani; Manga Vijjulatha
Journal:  Mol Divers       Date:  2020-05-02       Impact factor: 2.943

4.  Design, synthesis, DFT, docking studies and ADME prediction of some new coumarinyl linked pyrazolylthiazoles: Potential standalone or adjuvant antimicrobial agents.

Authors:  Sunil Kumar; Vikram Saini; Indresh K Maurya; Jayant Sindhu; Mukesh Kumari; Ramesh Kataria; Vinod Kumar
Journal:  PLoS One       Date:  2018-04-19       Impact factor: 3.240

5.  New pyrazolylpyrazoline derivatives as dual acting antimalarial-antileishamanial agents: synthesis, biological evaluation and molecular modelling simulations.

Authors:  Adnan A Bekhit; Eskedar T Lodebo; Ariaya Hymete; Hanan M Ragab; Salma A Bekhit; Kikuko Amagase; Afnan Batubara; Mohammed A S Abourehab; Alaa El-Din A Bekhit; Tamer M Ibrahim
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

6.  In Silico Design, Synthesis, and Biological Evaluation of Anticancer Arylsulfonamide Endowed with Anti-Telomerase Activity.

Authors:  Giulia Culletta; Mario Allegra; Anna Maria Almerico; Ignazio Restivo; Marco Tutone
Journal:  Pharmaceuticals (Basel)       Date:  2022-01-10

7.  Targeting telomerase with radiolabeled inhibitors.

Authors:  Philip A Waghorn; Mark R Jackson; Veronique Gouverneur; Katherine A Vallis
Journal:  Eur J Med Chem       Date:  2016-09-10       Impact factor: 7.088
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.