Design, Synthesis, and <i>In vitro</i> Evaluation of Thieno[a]dibenzothiophene Derivatives

Konuş, Metin; Algso, Muheb A. S.; Kavak, Emrah; Kurt‐Kızıldoğan, Aslıhan; Yılmaz, Can; Kıvrak, Arif

doi:10.1002/slct.202000685

Cited by 8 publications

(3 citation statements)

References 62 publications

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“…Heteroaromatic compounds have biologically important properties and because of this fact, they are the subject of many studies for drug discovery and development. [1] Those practices are carried out on sulfur-based heteroaromatic structures, especially thiophene derivatives, which are remarkable for their clinical potential to be used as antimicrobial, [2] insecticidal, [3] anticancer, [4] antioxidant [5,6] and antifungal [7] agents. Such heteroaromatic compounds have a significant place in the list of the most used drugs in the world pharmaceutical market.…”

Section: Introductionmentioning

confidence: 99%

A Thiophene Derivative, 2‐Bromo‐5‐(2‐(methylthio)phenyl)thiophene, Has Effective Anticancer Potential with Other Biological Properties

et al. 2022

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Thiophene derivatives are studied intensively due to their anticancer, antimicrobial, antioxidant and some other clinically important properties. In this study, the biological properties of a new thiophene derivative, so called BMPT, with a moderate drug score of 0.29 were tested. BMPT showed selective cytotoxicity for LnCap, HepG2 and Caco‐2 cancer cell lines with EC50 values of 138.573 μM, 185.931 μM, and 108.657 μM, respectively, but not on the control cell line HEK293. The increased expressions were detected for caspase3, caspase8, caspase9 and Bax; but Bcl‐2 expressions were decreased at cancer cell lines. BMPT decreased the total thiol content and total GST activities at HepG2 47 % and 40 %, respectively, and, molecular docking supported inhibitory models for GSTP1‐1, GSTA1‐1 and GSTM2‐2 were mixed, uncompetitive and uncompetitive, respectively. BMPT also showed potent antibacterial activity against Staphylococcus aureus. Related with its selective inhibition on GST activities, BMPT is proposed to have significant apoptotic effect leaded by changes, especially, in caspase 3, Bcl‐2 and Bax expressions.

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Section: Introductionmentioning

confidence: 99%

A Thiophene Derivative, 2‐Bromo‐5‐(2‐(methylthio)phenyl)thiophene, Has Effective Anticancer Potential with Other Biological Properties

et al. 2022

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“…Recently, we designed and synthesized novel benzothiophene derivatives via electrophilic cyclization reactions. It was investigated that sulfur and nitrogen atoms may be increased the biological properties or create new activities …”

Section: Introductionmentioning

confidence: 99%

“…It was investigated that sulfur and nitrogen atoms may be increased the biological properties or create new activities. [21] In the present study, novel indole derivatives, containing mono-and di-thiophene group, (3-(5-bromothiophen-2-yl)-1ethyl-2-phenyl-1H-indole 4 and 3-([2,2'-bithiophen]-5-yl)-1ethyl-2-phenyl-1H-indole 5) were synthesized by using coupling and electrophilic substitution reactions. We were mainly interested in exploring biological properties of these novel thiophene based indole derivatives.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Biological Evaluation and Molecular Docking of Novel Thiophene‐Based Indole Derivatives as Potential Antibacterial, GST Inhibitor and Apoptotic Anticancer Agents

et al. 2020

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Heteroaromatic indoles play a leading role in the development of pharmaceutical, medical, chemical and agricultural fields due to their structural properties. In this study, it was first time that biological properties of (antioxidant, antimicrobial, cytotoxic and apoptotis-induced anticancer) 3-(5-bromothiophen-2-yl)-1ethyl-2-phenyl-1H-indole 4 and 3-([2,2'-bithiophen]-5-yl)-1ethyl-2-phenyl-1H-indole 5 were described. According to the overall results, while 4 did not show any significant cytotoxic, antioxidant and antimicrobial activities, 5 showed high reduc-ing activity and very strong antibacterial activity against Enterococcus faecalis. Furthermore, 5 showed dose-dependent cytotoxic effect in all tested cell lines. The EC 50 values of the 5 were found to be 16 μM for CaCo-2, 29 μM for LnCaP, 14 μM for MDA-MB231, 21 μM for HepG2 and 87 μM for HEK293 cells, respectively. 5 also caused induction of apoptosis and promising glutathione S-transferase (GST) enzyme inhibition in HepG2 cells. Consequently, 5 could be also considered as a promising medical agent in cancer treatment.[a] Dr. M.

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New Thiophene–Butanol Derivatives: Synthesis, Spectroscopic Characterization, DFT, Biological Activities and In Silico Study

Ustabaş,

Süleymanoğlu,

Çelik

et al. 2023

Russ. J. Phys. Chem.

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Design, Synthesis, and In vitro Evaluation of Thieno[a]dibenzothiophene Derivatives

Cited by 8 publications

References 62 publications

A Thiophene Derivative, 2‐Bromo‐5‐(2‐(methylthio)phenyl)thiophene, Has Effective Anticancer Potential with Other Biological Properties

A Thiophene Derivative, 2‐Bromo‐5‐(2‐(methylthio)phenyl)thiophene, Has Effective Anticancer Potential with Other Biological Properties

Synthesis, Biological Evaluation and Molecular Docking of Novel Thiophene‐Based Indole Derivatives as Potential Antibacterial, GST Inhibitor and Apoptotic Anticancer Agents

New Thiophene–Butanol Derivatives: Synthesis, Spectroscopic Characterization, DFT, Biological Activities and In Silico Study

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