scholarly journals Synthesis and biological evaluation of 6-substituted indolizinoquinolinediones as catalytic DNA topoisomerase I inhibitors

2015 ◽  
Vol 101 ◽  
pp. 525-533 ◽  
Author(s):  
Le-Mao Yu ◽  
Xiao-Ru Zhang ◽  
Xiao-Bing Li ◽  
Yuan Yang ◽  
Hong-Yu Wei ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Biological Evaluation ◽  
Dna Topoisomerase I ◽  
Dna Topoisomerase ◽  
Topoisomerase I Inhibitors ◽  
Catalytic Dna ◽  
Synthesis And Biological Evaluation

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.

Synthesis and Pharmacological Evaluation of Novel Homocamptothecin-Dihydropyridine Derivative Conjugates as Potent Topoisomerase I Inhibitors

2011 ◽  
Vol 64 (10) ◽  
pp. 1390 ◽  
Author(s):  
Ling-Jian Zhu ◽  
Chun-Lin Zhuang ◽  
Ning Lei ◽  
Chun-Quan Sheng ◽  
Wei Guo ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Antitumour Activity ◽  
Tumour Cell Line ◽  
Dna Topoisomerase I ◽  
Inhibition Activity ◽  
Dna Topoisomerase ◽  
Antitumour Agents ◽  
Topoisomerase I Inhibitors ◽  
Dihydropyridine Derivative ◽  
New Generation

Homocamptothecins (hCPT) represent a new generation of antitumour agents targeting DNA topoisomerase I. The expanded seven-membered lactone E-ring that characterizes hCPT enhances the plasma stability of the drug and reinforces the inhibition of topoisomerase I (Topo I) compared with conventional six-membered CPT. In an attempt to improve the antitumour activity of hCP, a series of novel hCPT derivatives conjugating with dihydropyridine derivates were designed and synthesized based on a synthetic route that couples 7-formylhomocamptothecin with different dihydropyridine derivates. Most of the synthesized compounds exhibited good cytotoxic activity on tumour cell line A549, MDA-MB-435, and HCT116. Furthermore, this class of compounds showed superior Topo I inhibition activity comparable to or higher than CPT.

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