scholarly journals Identification and biological evaluation of novel benzothiazole derivatives bearing a pyridine-semicarbazone moiety as apoptosis inducers via activation of procaspase-3 to caspase-3

MedChemComm ◽  
2019 ◽  
Vol 10 (3) ◽  
pp. 465-477 ◽  
Author(s):  
Junjie Ma ◽  
Xin Ni ◽  
Yali Gao ◽  
Kun Huang ◽  
Jiaan Liu ◽  
...  
Keyword(s):  
Caspase 3 ◽  
Biological Evaluation ◽  
Benzothiazole Derivatives

A series of benzothiazole derivatives bearing a pyridine-semicarbazone moiety were identified as apoptosis inducers via activation of procaspase-3 to caspase-3.

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.

Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents

2005 ◽  
Vol 15 (14) ◽  
pp. 3328-3332 ◽  
Author(s):  
Masao Yoshida ◽  
Ichiro Hayakawa ◽  
Noriyuki Hayashi ◽  
Toshinori Agatsuma ◽  
Youko Oda ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Benzothiazole Derivatives ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of novel 1,2-benzisothiazol-3-one-derived 1,2,3-triazoles as caspase-3 inhibitors

2014 ◽  
Vol 24 (5) ◽  
pp. 1814-1829 ◽  
Author(s):  
Zhenfei Guo ◽  
Zhihui Yan ◽  
Xiaowei Zhou ◽  
Quan Wang ◽  
Meiqi Lu ◽  
...  
Keyword(s):  
Caspase 3 ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of Heteroaryldiamides and Heteroaryldiamines as Cytotoxic Agents, Apoptosis Inducers and Caspase-3 Activators

2006 ◽  
Vol 339 (4) ◽  
pp. 182-192 ◽  
Author(s):  
Mikel Echeverría ◽  
Beatriz Mendívil ◽  
Lucía Cordeu ◽  
Elena Cubedo ◽  
Jesús García-Foncillas ◽  
...  
Keyword(s):  
Caspase 3 ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis, spectral studies and biological activity of 2, 3-disubstituted imidazo [2, 1-b] benzothiazole derivatives

2018 ◽  
Vol 6 (01) ◽  
pp. 01-08
Author(s):  
Yashveer Singh ◽  
Baljeet Kaur ◽  
Amandeep Kaur ◽  
Vivek Kumar Gupta ◽  
Monika Gupta
Keyword(s):  
Antimicrobial Activity ◽  
Catalytic Domain ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Thiazole Ring ◽  
Standard Drug ◽  
Atp Binding Site ◽  
Benzothiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

Benzothiazole is a heterocyclic compound formed by the fusion of benzene and thiazole ring. The moiety had been reported to act via competing with ATP binding site at the catalytic domain of tyrosine kinase. The present work involves the synthesis and biological evaluation of 4, 5 disubstituted imidazo [2, 1-b] benzothiazole derivatives. The antimicrobial activity of the synthesized derivatives was carried out against Gram + ve bacteria Staphylococcus aureus (MTCC 3160) and Gram –ve bacteria Bordetella bronchiseptica (MTCC 6838), Pseudomonas aeruginosa (T11) and fungal strains Candida albicans (MTCC 1637). Ciprofloxacin and Fluconazole were used as standard drug for antibacterial and antifungal activity respectively. The compounds 6a1, 6a2, 6a3, 6b1 and 8a1 exhibited good antimicrobial activity against all the strains. The derivative 8a1 was further screened for anticancer activity against MCF-7 cell line using Doxorubicin as standard. The structures of the synthesized compounds were established by IR and NMR spectral studies.

Design, synthesis, biological evaluation and docking studies of sulfonyl isatin derivatives as monoamine oxidase and caspase-3 inhibitors

MedChemComm ◽  
2016 ◽  
Vol 7 (8) ◽  
pp. 1628-1639 ◽  
Author(s):  
Mohsen Tavari ◽  
Sarel F. Malan ◽  
Jacques Joubert
Keyword(s):  
Monoamine Oxidase ◽  
Caspase 3 ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Multifunctional Agents ◽  
Inhibitory Activities ◽  
Isatin Derivatives ◽  
Micromolar Range

Sulfonyl isatin derivatives as multifunctional agents showing monoamine oxidase and caspase-3 inhibitory activities in the low micromolar range.

Design, Synthesis, and Biological Evaluation of Isoquinoline-1,3,4-trione Derivatives as Potent Caspase-3 Inhibitors

2006 ◽  
Vol 49 (5) ◽  
pp. 1613-1623 ◽  
Author(s):  
Yi-Hua Chen ◽  
Ya-Hui Zhang ◽  
Hua-Jie Zhang ◽  
Da-Zhi Liu ◽  
Min Gu ◽  
...  
Keyword(s):  
Caspase 3 ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
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