Design and Synthesis of New [1,2,3]Triazolo[4,5-d]pyrimidine Derivatives as Potential Antiproliferative Agents

2015 ◽  
Vol 36 (7) ◽  
pp. 1863-1873 ◽  
Author(s):  
Ahmed Elkamhawy ◽  
Mohammad M. Al-Sanea ◽  
Chiman Song ◽  
Taebo Sim ◽  
Eun Joo Roh
Keyword(s):  
Pyrimidine Derivatives ◽  
Antiproliferative Agents ◽  
Design And Synthesis

scholarly journals Design and Synthesis of (2-oxo-1,2-Dihydroquinolin-4-yl)-1,2,3-triazole Derivatives via Click Reaction: Potential Apoptotic Antiproliferative Agents

Molecules ◽  
2021 ◽  
Vol 26 (22) ◽  
pp. 6798
Author(s):  
Essmat M. El-Sheref ◽  
Mohammed A. I. Elbastawesy ◽  
Alan B. Brown ◽  
Ahmed M. Shawky ◽  
Hesham A. M. Gomaa ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Click Reaction ◽  
Annexin V ◽  
Antiproliferative Agents ◽  
Design And Synthesis ◽  
Cycle Arrest ◽  
M Phase ◽  
Reaction Potential ◽  
Apoptotic Activity ◽  
Mcf 7

A mild and versatile method based on Cu-catalyzed [2+3] cycloaddition (Huisgen-Meldal-Sharpless reaction) was developed to tether 3,3’-((4-(prop-2-yn-1-yloxy)phenyl)methylene)bis(4-hydroxyquinolin-2(1H)-ones) with 4-azido-2-quinolones in good yields. This methodology allowed attaching three quinolone molecules via a triazole linker with the proposed mechanism. The products are interesting precursors for their anti-proliferative activity. Compound 8g was the most active one, achieving IC50 = 1.2 ± 0.2 µM and 1.4 ± 0.2 µM against MCF-7 and Panc-1 cell lines, respectively. Moreover, cell cycle analysis of cells MCF-7 treated with 8g showed cell cycle arrest at the G2/M phase (supported by Caspase-3,8,9, Cytochrome C, BAX, and Bcl-2 studies). Additionally, significant pro-apoptotic activity is indicated by annexin V-FITC staining.

New pyrazolo-triazolo-pyrimidine derivatives as antibacterial agents: Design and synthesis, molecular docking and DFT studies

2020 ◽  
Vol 1199 ◽  
pp. 127007 ◽  
Author(s):  
Mabrouk Horchani ◽  
Amel Hajlaoui ◽  
Abdel Halim Harrath ◽  
Lamjed Mansour ◽  
Hichem Ben Jannet ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antibacterial Agents ◽  
Dft Studies ◽  
Pyrimidine Derivatives ◽  
Design And Synthesis

scholarly journals Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer

2016 ◽  
Vol 118 ◽  
pp. 230-243 ◽  
Author(s):  
Marcella Bassetto ◽  
Salvatore Ferla ◽  
Fabrizio Pertusati ◽  
Sahar Kandil ◽  
Andrew D. Westwell ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Antiproliferative Agents ◽  
Design And Synthesis

ChemInform Abstract: Design and Synthesis of 2-Iminothiazolidin-4-one Moiety-Containing Compounds as Potent Antiproliferative Agents.

ChemInform ◽  
2012 ◽  
Vol 43 (37) ◽  
pp. no-no
Author(s):  
Xin Zhai ◽  
Wei Li ◽  
Dong Chen ◽  
Ruiwei Lai ◽  
Jun Liu ◽  
...  
Keyword(s):  
Antiproliferative Agents ◽  
Design And Synthesis

Design and synthesis of novel 4-hydrazone functionalized/1,2,4-triazole fused pyrido[2,3-d]pyrimidine derivatives, their evaluation for antifungal activity and docking studies

2019 ◽  
Vol 28 (9) ◽  
pp. 1509-1528
Author(s):  
Nooka Ratnam Appna ◽  
Ravi Kumar Nagiri ◽  
Raghu Babu Korupolu ◽  
Sirisha Kanugala ◽  
Ganesh Kumar Chityal ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Docking Studies ◽  
Pyrimidine Derivatives ◽  
Design And Synthesis

Design and synthesis of novel N,N′-glycoside derivatives of 3,3′-diindolylmethanes as potential antiproliferative agents

MedChemComm ◽  
2012 ◽  
Vol 3 (9) ◽  
pp. 1082 ◽  
Author(s):  
Deepak K. Sharma ◽  
Bilal Rah ◽  
Mallikharjuna R. Lambu ◽  
Altaf Hussain ◽  
Syed K. Yousuf ◽  
...  
Keyword(s):  
Antiproliferative Agents ◽  
Design And Synthesis ◽  
Derivatives Of

scholarly journals Design, synthesis, and biological evaluation of new thiazolo[5,4-d]pyrimidine derivatives as potent antiproliferative agents

MedChemComm ◽  
2017 ◽  
Vol 8 (8) ◽  
pp. 1655-1658 ◽  
Author(s):  
Zhong-Hua Li ◽  
Xue-Qi Liu ◽  
Peng-Fei Geng ◽  
Jin-Lian Ma ◽  
Tao-Qian Zhao ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Pyrimidine Derivative ◽  
Pyrimidine Derivatives ◽  
Design Synthesis ◽  
Antiproliferative Agents ◽  
Potent Inhibition ◽  
Synthesis And Biological Evaluation

The thiazolo[5,4-d]pyrimidine derivative 7i exhibited potent inhibition against MGC-803 and HGC-27 with IC50 values of 4.64 and 5.07 μM, respectively and around 12-fold selectivity between MGC-803 and GES-1.

Design and synthesis of new 2-anilinoquinolines bearing N -methylpicolinamide moiety as potential antiproliferative agents

2016 ◽  
Vol 89 (1) ◽  
pp. 98-113 ◽  
Author(s):  
Ashraf Kareem El-Damasy ◽  
Seon Hee Seo ◽  
Nam-Chul Cho ◽  
Ae Nim Pae ◽  
Eunice Eunkyeong Kim ◽  
...  
Keyword(s):  
Antiproliferative Agents ◽  
Design And Synthesis
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