Amphimic acids and related long-chain fatty acids as DNA topoisomerase I inhibitors from an Australian sponge, Amphimedon sp.: Isolation, structure, synthesis, and biological evaluation

Tetrahedron ◽  
1997 ◽  
Vol 53 (49) ◽  
pp. 16699-16710 ◽  
Author(s):  
Takayuki Nemoto ◽  
Go Yoshino ◽  
Makoto Ojika ◽  
Youji Sakagami
Keyword(s):  
Fatty Acids ◽  
Topoisomerase I ◽  
Biological Evaluation ◽  
Dna Topoisomerase I ◽  
Long Chain Fatty Acids ◽  
Dna Topoisomerase ◽  
Topoisomerase I Inhibitors ◽  
Structure Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Long Chain

Synthesis and Biological Evaluation of 1,5-Naphthyridines as Topoisomerase I Inhibitors. A New Family of Antiproliferative Agents

2015 ◽  
Vol 14 (23) ◽  
pp. 2722-2728 ◽  
Author(s):  
Concepcion Alonso ◽  
Maria Fuertes ◽  
Maria Gonzalez ◽  
Alicia Rodriguez-Gascon ◽  
Gloria Rubiales ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Biological Evaluation ◽  
Antiproliferative Agents ◽  
Topoisomerase I Inhibitors ◽  
New Family ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of Some 1,8-Naphthalimide-Acridinyl Hybrids

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Rui Chen ◽  
Caiying Yuan ◽  
Yogini Jaiswal ◽  
Lini Huo ◽  
Dianpeng Li ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Inhibition Activity ◽  
Dna Topoisomerase ◽  
Human Cancer Cell Lines ◽  
Pharmacological Mechanism ◽  
Electrophorus Electricus ◽  
Synthesis And Biological Evaluation ◽  
Mcf 7

In the present study, the synthesis of three 1,8-naphthalimide-acridinyl hybrids (2a, 2b, and 5b) using N-amido-1,8-naphthalimides (1 and 4) and acridinyl isothiocyanates is reported. The newly synthesized hybrids were evaluated for their anticancer activity in six human cancer cell lines (HL-60, MT-4, HepG2, HeLa, SK-OV-3, and MCF-7). Their inhibition activity against DNA-topoisomerase I (Topo I) and Electrophorus electricus acetylcholinesterase (AChE) was also studied. The results indicate that 2b displayed good cytotoxicity for MT-4, HepG2, HeLa, and SK-OV-3 with the IC50 values of 14.66 ± 0.31, 27.32 ± 2.67, 17.51 ± 0.34, and 32.26 ± 1.74 μM, respectively. All compounds, especially 2b, exhibited obvious bands corresponding to DNA fragments at 0.5 mM concentration, further confirming the pharmacological mechanism related to the Topo I inhibitory activities. In addition, compound 2a exhibited higher inhibition activity against AChE than 2b and 5b, with IC50 values of 0.32 ± 0.04 mM, and the acridinyl ring may contribute to the activity of 2a.

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