scholarly journals Benzimidazole-1,2,3-triazole hybrid molecules: synthesis and study of their interaction with G-quadruplex DNA

2021 ◽  
Author(s):  
Padma S. Singu ◽  
Ushasri Chilakamarthi ◽  
Namita S. Mahadik ◽  
Bhamidipati Keerti ◽  
Narasimhulu Valipenta ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Activity ◽  
Duplex Dna ◽  
Quadruplex Dna ◽  
Hybrid Molecules ◽  
G Quadruplex ◽  
M Phase

The benzimidazole-1,2,3-triazole hybrid 4f selectively interacted with G-quadruplex DNA over duplex DNA, inhibits cell cycle at the G2/M phase, inducing apoptosis, and may be a G-quadruplex DNA groove binder with anticancer activity.

Multicarbazole scaffolds for selective G-quadruplex binding

2018 ◽  
Vol 54 (69) ◽  
pp. 9647-9650 ◽  
Author(s):  
Arnold Ou ◽  
Aurore Guédin ◽  
Brian W. Skelton ◽  
Samir Amrane ◽  
Cameron W. Evans ◽  
...  
Keyword(s):  
Duplex Dna ◽  
Quadruplex Dna ◽  
G Quadruplex

N-Functionalised multicarbazoles were found to be highly selective towards G-quadruplex DNA in the presence of 250× excess duplex DNA competitor.

scholarly journals Synthesis and Biological Evaluation of Benzodioxole Derivatives as Potential Anticancer and Antioxidant agents

2020 ◽  
Vol 26 (1) ◽  
pp. 157-167
Author(s):  
Mohammed Hawash ◽  
Ahmad M Eid ◽  
Nidal Jaradat ◽  
Murad Abualhasan ◽  
Johnny Amer ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Activity ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Antioxidant Agents ◽  
M Phase ◽  
Benzodiazepine Derivatives ◽  
Antioxidant Agent ◽  
Synthesis And Biological Evaluation

Abstracta series of benzodioxole compounds were synthesized and evaluated for their cytotoxic activity against cervical (Hela), colorectal (Caco-2), and liver (Hep3B) cancer cell lines. Compounds 5a, 5b, 6a, 6b, 7a and 7b showed very weak or negligible anticancer activity with IC50 3.94-9.12 mM. On the contrary, carboxamide containing compounds 2a and 2b showed anticancer activity. Both 2a and 2b reduced Hep3B secretions of α-fetoprotein (α-FP) to 1625.8 ng/ml and 2340 ng/ml, respectively, compared to 2519.17 ng/ml in untreated cells. The results also showed that compound 2a has potent anticancer activity against Hep3B cancer cell line. Furthermore, in cell cycle analysis, compound 2a induced arrest in the G2-M phase in value of 8.07% that was very close to the activity of doxorubicin (7.4%). These results indicate that compound 2a has a potent and promising antitumor activity. However, benzodiazepine derivatives (7a and 7b) showed moderate antioxidant activity with IC50 values of 39.85 and 79.95 μM, respectively compared with the potent antioxidant agent Trolox (IC50 = 7.72 μM).

Benzofuroquinoline Derivatives Had Remarkable Improvement of their Selectivity for Telomeric G-Quadruplex DNA over Duplex DNA upon Introduction of Peptidyl Group

2012 ◽  
Vol 23 (9) ◽  
pp. 1821-1831 ◽  
Author(s):  
Yi Long ◽  
Zeng Li ◽  
Jia-Heng Tan ◽  
Tian-Miao Ou ◽  
Ding Li ◽  
...  
Keyword(s):  
Duplex Dna ◽  
Quadruplex Dna ◽  
Remarkable Improvement ◽  
G Quadruplex

Identification of a selective G-quadruplex DNA binder using a multistep virtual screening approach

2015 ◽  
Vol 51 (1) ◽  
pp. 198-201 ◽  
Author(s):  
Jin-Qiang Hou ◽  
Shuo-Bin Chen ◽  
Li-Peng Zan ◽  
Tian-Miao Ou ◽  
Jia-Heng Tan ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Duplex Dna ◽  
Quadruplex Dna ◽  
Screening Approach ◽  
G Quadruplex ◽  
Virtual Screening Approach

A selective G-quadruplex binder was identified using a multistep virtual screening approach by simultaneously taking into account G-quadruplex and duplex DNA.

Stabilization for loop isomers of c-myc G-quadruplex DNA and anticancer activity by ruthenium complexes

MedChemComm ◽  
2014 ◽  
Vol 5 (11) ◽  
pp. 1724-1728 ◽  
Author(s):  
Ying Liu ◽  
Yanan Liu ◽  
Licong Yang ◽  
Chengwen Cao ◽  
Yanhui Zhou ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Ruthenium Complexes ◽  
Quadruplex Dna ◽  
G Quadruplex

New 2,9-disubstituted-1,10-phenanthroline derivatives with anticancer activity by selective targeting of telomeric G-quadruplex DNA

2021 ◽  
Vol 249 ◽  
pp. 119318
Author(s):  
Anda-Mihaela Craciun ◽  
Alexandru Rotaru ◽  
Corneliu Cojocaru ◽  
Ionel I. Mangalagiu ◽  
Ramona Danac
Keyword(s):  
Anticancer Activity ◽  
Quadruplex Dna ◽  
Selective Targeting ◽  
G Quadruplex

Synthesis, Antitumor Activity and Molecular Docking Studies on Seven Novel Thiazacridine Derivatives

2020 ◽  
Vol 23 (5) ◽  
pp. 359-368
Author(s):  
Marcel L. Almeida ◽  
Douglas C.F. Viana ◽  
Valécia C.M. da Costa ◽  
Flaviana A. dos Santos ◽  
Michelly C. Pereira ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cell Cycle ◽  
Molecular Docking ◽  
Anticancer Activity ◽  
Tumor Cells ◽  
Therapeutic Potential ◽  
Lymphoblastic Leukemia ◽  
Myelogenous Leukemia ◽  
Chemical Structures ◽  
Hybrid Molecules

Aim and Objective: In the last decades, cancer has become a major problem in public health all around the globe. Chimeric chemical structures have been established as an important trend on medicinal chemistry in the last years. Thiazacridines are hybrid molecules composed of a thiazolidine and acridine nucleus, both pharmacophores that act on important biological targets for cancer. By the fact it is a serious disease, seven new 3-acridin-9-ylmethyl-thiazolidine-2,4-dione derivatives were synthesized, characterized, analyzed by computer simulation and tested in tumor cells. In order to find out if the compounds have therapeutic potential. Materials and Methods: Seven new 3-acridin-9-ylmethyl-thiazolidine-2,4-dione derivatives were synthesized through Michael addition and Knoevenagel condensation strategies. Characterization was performed by NMR and Infrared spectroscopy techniques. Regarding biological activity, thiazacridines were tested against solid and hematopoietic tumoral cell lines, namely Jurkat (acute T-cell leukemia); HL-60 (acute promyelocytic leukemia); DU 145 (prostate cancer); MOLT-4 (acute lymphoblastic leukemia); RAJI (Burkitt's lymphoma); K562 (chronic myelogenous leukemia) and normal cells PBMC (healthy volunteers). Molecular docking analysis was also performed in order to assess major targets of these new compounds. Cell cycle and clonogenic assay were also performed. Results: Compound LPSF/AA-62 (9f) exhibited the most potent anticancer activity against HL-60 (IC50 3,7±1,7 μM), MOLT-4 (IC50 5,7±1,1 μM), Jurkat (IC50 18,6 μM), Du-145 (IC50 20±5 μM) and Raji (IC50 52,3±9,2 μM). While the compound LPSF/AA-57 (9b) exhibited anticancer activity against the K562 cell line (IC50 51,8±7,8 μM). Derivative LPSF/AA-62 (9f) did not interfere in the cell cycle phases of the Molt-4 lineage. However, the LPSF/AA-62 (9f) derivative significantly reduced the formation of prostate cancer cell clones. The compound LPSF/AA-62 (9f) has shown strong anchorage stability with enzymes topoisomerases 1 and 2, in particular due the presence of chlorine favored hydrogen bonds with topoisomerase 1. Conclusion: The 3-(acridin-9-ylmethyl)-5-((10-chloroanthracen-9-yl)methylene)thiazolidine-2,4-dione (LPSF/AA-62) presented the most promising results, showing anti-tumor activity in 5 of the 6 cell types tested, especially inhibiting the formation of colonies of prostate tumor cells (DU-145).

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