Design, synthesis, and biological evaluation of novel benzimidazole derivatives as sphingosine kinase 1 inhibitor

2021 ◽  
Author(s):  
Sarah H. M. Khairat ◽  
Mohamed A. Omar ◽  
Fatma A. F. Ragab ◽  
Sonam Roy ◽  
Ahmad A. Turab Naqvi ◽  
...  
Keyword(s):  
Sphingosine Kinase ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Sphingosine Kinase 1 ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of some novel benzimidazole derivatives for their potential anticonvulsant activity

2010 ◽  
Vol 33 (7) ◽  
pp. 971-980 ◽  
Author(s):  
Priyal Jain ◽  
Prakash Kumar Sharma ◽  
Harish Rajak ◽  
Rajesh Singh Pawar ◽  
Umesh Kumar Patil ◽  
...  
Keyword(s):  
Anticonvulsant Activity ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals In Silico Studies, Synthesis and Biological Evaluation of 4,5-Dehydrospisulosine Butyrate Ceramides as Potential Sphingosine Kinase I Inhibitors

2021 ◽  
Author(s):  
Parleen Kaur ◽  
Sonia Sharma ◽  
Vinay Randhawa ◽  
Navneet Agnihotri ◽  
Ramandeep Kaur ◽  
...  
Keyword(s):  
Evaluation Studies ◽  
Docking Simulation ◽  
Sphingosine Kinase ◽  
Biological Evaluation ◽  
High Yield ◽  
Binding Affinities ◽  
Sphingosine Kinase 1 ◽  
Molecular Docking Simulation ◽  
In Silico Studies ◽  
Synthesis And Biological Evaluation

Abstract In the present work, synthesis of 4,5-dehydrospiulosine and its chain analogues (1-3) as potential Sphingosine Kinase I inhibitors has been achieved via the diasteroselective Grignard reaction, stereoselective cross metathesis reaction followed by N-acylation with p-nitrophenyl butyrate to give the corresponding butyrate ceramides (4-6). All compounds were obtained in high yield and purity followed by molecular docking simulation studies using AutoDock which indicated their varying binding affinities with Sphingosine Kinase 1 protein was done. Further, the biological evaluation studies, as potential anti-prostate cancer agents by inhibiting the sphingosine kinase 1 protien of all synthesized compounds (1-6) on PC-3 cell lines by SRB method was done. Compound N-((2S,3S,E)-3 hydroxyheptadec-4-en-2-yl) butyramide (4) exhibited remarkable cytotoxicity with an IC50 value of 6.06 µM.

scholarly journals Design, synthesis and biological evaluation of 3′,4′,5′-trimethoxy flavonoid benzimidazole derivatives as potential anti-tumor agents

MedChemComm ◽  
2018 ◽  
Vol 9 (2) ◽  
pp. 305-315 ◽  
Author(s):  
Zhe Wang ◽  
Xiangping Deng ◽  
Runde Xiong ◽  
Shujuan Xiong ◽  
Juan Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

A series of 3′,4′,5′-trimethoxy flavonoids with benzimidazole linked by different chain alkanes have been designed and synthesized.

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