scholarly journals Synthesis and biological evaluation of fluoro-substituted spiro-isoxazolines as potential anti-viral and anti-cancer agents

RSC Advances ◽  
2020 ◽  
Vol 10 (50) ◽  
pp. 30223-30237
Author(s):  
Prasanta Das ◽  
Sarah Boone ◽  
Dipanwita Mitra ◽  
Lindsay Turner ◽  
Ritesh Tandon ◽  
...  

The synthetic efficacy and biological relevance extend an opportunity to further drug-discovery development of fluoro-spiro-isoxazolines as novel anti-viral and anti-cancer agents.

2017 ◽  
Vol 27 (9) ◽  
pp. 1923-1928 ◽  
Author(s):  
Suresh Poudapally ◽  
Shankar Battu ◽  
Loka Reddy Velatooru ◽  
Murali Satyanarayana Bethu ◽  
Venkateswara Rao Janapala ◽  
...  

2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC50>79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC50=65.3μM), it indeed significantly abrogated endothelia cell migration (IC50=6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.


2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.0 2,6 ] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1 H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC 50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC 50 > 79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC 50 =65.3μM), it indeed significantly abrogated endothelia cell migration (IC 50 =6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.


RSC Advances ◽  
2017 ◽  
Vol 7 (38) ◽  
pp. 23265-23271 ◽  
Author(s):  
Kaili Jia ◽  
Xinxin Lv ◽  
Dong Xing ◽  
Jiuwei Che ◽  
Donglan Liu ◽  
...  

A series of substituted 3-amino-3-hydroxymethyloxindoles synthesized through a multi-component approach showed anticancer potency. The most potent compound 5m inhibits SJSA-1 proliferation with an IC50 of 3.14 μM. It can also induce time- and dose-dependent apoptosis.


2012 ◽  
Vol 22 (23) ◽  
pp. 7268-7271 ◽  
Author(s):  
Tianwen Li ◽  
Yongchong Yang ◽  
Changmei Cheng ◽  
Amit K. Tiwari ◽  
Kamlesh Sodani ◽  
...  

2018 ◽  
Vol 80 ◽  
pp. 631-638 ◽  
Author(s):  
Sina Omid Malayeri ◽  
Zahra Tayarani-Najaran ◽  
Fatemeh Shaebani Behbahani ◽  
Roghayeh Rashidi ◽  
Saeedeh Delpazir ◽  
...  

2018 ◽  
Vol 26 (4) ◽  
pp. 884-890 ◽  
Author(s):  
Cornelis P. Vlaar ◽  
Linette Castillo-Pichardo ◽  
Julia I. Medina ◽  
Cathyria M. Marrero-Serra ◽  
Ericka Vélez ◽  
...  

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