Design, Synthesis and Bio-evaluation of New Phenothiazine Derivatives of Sulfonamide Dyes as Anticancer Agents

2020 ◽  
Vol 5 (3) ◽  
pp. 20030406-20030406
Author(s):  
Manoj D. Shanti
Keyword(s):  
Anticancer Agents ◽  
Phenothiazine Derivatives ◽  
Design Synthesis ◽  
Sulfonamide Dyes ◽  
Derivatives Of

Hybridized Quinoline Derivatives as Anticancer Agents: Design, Synthesis, Biological Evaluation and Molecular Docking

2019 ◽  
Vol 19 (4) ◽  
pp. 439-452 ◽  
Author(s):  
Mohamed R. Selim ◽  
Medhat A. Zahran ◽  
Amany Belal ◽  
Moustafa S. Abusaif ◽  
Said A. Shedid ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Caspase 3 ◽  
Biological Evaluation ◽  
Tubulin Polymerization ◽  
Design Synthesis ◽  
Chemical Structures ◽  
M Phase ◽  
Induced Apoptosis ◽  
Derivatives Of

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

Three Amino Acid Derivatives of Valproic Acid: Design, Synthesis, Theoretical and Experimental Evaluation as Anticancer Agents

2014 ◽  
Vol 14 (7) ◽  
pp. 984-993 ◽  
Author(s):  
Gabriela Luna-Palencia ◽  
Federico Martinez-Ramos ◽  
Ismael Vasquez-Moctezuma ◽  
Manuel Fragoso-Vazquez ◽  
Jessica Mendieta-Wejebe ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Amino Acid ◽  
Anticancer Agents ◽  
Experimental Evaluation ◽  
Amino Acid Derivatives ◽  
Design Synthesis ◽  
Derivatives Of

Amide derivatives of 4-azaindole: Design, synthesis, and EGFR targeting anticancer agents

2019 ◽  
Vol 50 (1) ◽  
pp. 71-84 ◽  
Author(s):  
Puli Venkat Swamy ◽  
Vukoti Kiran Kumar ◽  
Ruddarraju Radhakrishnam Raju ◽  
Regalla Venkata Reddy ◽  
Anindita Chatterjee ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Design Synthesis ◽  
Amide Derivatives ◽  
Derivatives Of

scholarly journals Design, Synthesis, and Cytotoxic Evaluation of Novel Lupane Triterpenoid Derived Hydroxamates

2020 ◽  
Vol 15 (6) ◽  
pp. 1934578X2093196
Author(s):  
Dang Thi Tuyet Anh ◽  
Dinh Thi Cuc ◽  
Le Nhat Thuy Giang ◽  
Nguyen Thi Hien ◽  
Vu Ngoc Doan ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Lupane Triterpenoids ◽  
Lead Compounds ◽  
Diphenyltetrazolium Bromide ◽  
Derivatives Of

A series of new hydroxamate derivatives of lupane triterpenoids has been designed and successfully synthesized. The synthesized compounds were evaluated for their in vitro antitumor activity using the 3-[4,5-dimethylthiazol-2-yl]−2,5-diphenyltetrazolium bromide-based assay against the human cancer cell lines KB and HepG2. Most of these derivatives possess at least moderate cytotoxic activity and the hydroxamate derivative compounds 3c, 3e, 7a, and 15b could be lead compounds for further optimization to develop novel anticancer agents.

Design, synthesis and biological evaluation of rhein derivatives as anticancer agents

MedChemComm ◽  
2016 ◽  
Vol 7 (9) ◽  
pp. 1812-1818 ◽  
Author(s):  
Junkai Huang ◽  
Zhuo Zhang ◽  
Peng Huang ◽  
Liqin He ◽  
Yong Ling
Keyword(s):  
Tumor Cell ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Promising Candidate ◽  
Design Synthesis ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel derivatives of rhein were synthesized and evaluated for their in vitro antiproliferative activity against six kinds of tumor cell lines. All derivatives displayed more potent anti-tumor activity than rhein, and most of them were even stronger than 5-FU. Compound 4v was the most promising candidate among the investigated compounds.

Design, synthesis and biological evaluation of sulphonamide derivatives of benzofuran-imidazopyridines as anticancer agents

2021 ◽  
Vol 31 ◽  
pp. 100608
Author(s):  
Indraganti Sreenivasa Murthy ◽  
Reddymasu Sireesha ◽  
Kolli Deepti ◽  
P. Srinivasa Rao ◽  
R. Ramesh Raju
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Design, Synthesis and Evaluation of Novel Derivatives of Orotic Acid Amide as Potent Glucokinase Activators

2017 ◽  
Vol 14 (3) ◽  
pp. 252-261 ◽  
Author(s):  
Leilei Zhang ◽  
Shengquan Hu ◽  
Lei Lei ◽  
Yuliang Zhang ◽  
Lijing Zhang ◽  
...  
Keyword(s):  
Orotic Acid ◽  
Acid Amide ◽  
Design Synthesis ◽  
Glucokinase Activators ◽  
Derivatives Of
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