Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents

Saravanan, K.; Elancheran, R.; Divakar, S.; Anand, S. Athavan Alias; Ramanathan, Meena; Kotoky, Jibon; Lokanath, N.K.; Kabilan, S.

doi:10.1016/j.bmcl.2017.01.065

Cited by 30 publications

(13 citation statements)

References 17 publications

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“…As described earlier, the western blotting analysis was carried out and is shown in Figure S7. The androgen significantly increased the protein expression of AR (~1.2 fold) and p-AR 213 (~1.4 fold), compared to the control (Saravanan et al, 2017). Bicalutamide and 6g significantly decreased the androgen-stimulated AR and p-AR protein expression.…”

Section: Resultsmentioning

confidence: 96%

RETRACTED: Design, Synthesis, and Biological Evaluation of (E)-N'-((1-Chloro-3,4-Dihydronaphthalen-2-yl)Methylene)Benzohydrazide Derivatives as Anti-prostate Cancer Agents

Arjun

Elancheran

Manikandan³

et al. 2019

Front. Chem.

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Prostate Cancer (PCa) is the most frequently diagnosed cancer in men in their late '50s. PCa growth is mainly due to the activation of the androgen receptor by androgens. The treatment for PCa may involve surgery, hormonal therapy, and oral chemotherapeutic drugs. A structural based molecular docking approach revealed the findings of (E)-N'-((1-chloro-3,4-dihydronaphthalen-2-yl)methylene)benzohydrazide derivatives, where the possible binding modes of the compounds with protein (PDB ID: 3V49) are shown. The compounds ( 6a-k ) were synthesized and characterized by using conventional methods. The compounds, 6g, 6j , and 6k were reconfirmed through single crystal X-ray diffraction (XRD). Further, the compounds (6a-k) and standard drug were evaluated against human prostate cancer cell lines, LNCaP and PC-3 and the non-cancerous cell line, 3T3. Among these compounds, 6g and 6j showed higher cytotoxicity, and 6g exhibited dose-dependent activity and reduced cell viability. The mechanism of action was observed through the induced apoptosis and was further confirmed by western blot and ELISA. Molecular dynamics simulation studies were carried out to calculate the interaction and the stability of the protein-ligand complex in motion. ADME properties were predicted for all the tested compounds. These findings may give vital information for further development.

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Section: Resultsmentioning

confidence: 96%

RETRACTED: Design, Synthesis, and Biological Evaluation of (E)-N'-((1-Chloro-3,4-Dihydronaphthalen-2-yl)Methylene)Benzohydrazide Derivatives as Anti-prostate Cancer Agents

Arjun

Elancheran

Manikandan³

et al. 2019

Front. Chem.

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“…Another example showing the effectiveness of copper complexes in order to inhibit the bacterial growth is related to the synthesis of a phthalimide-based copper(II) complex 5 [43]. Due to their planar aromatic rings, phthalimide moieties and derivatives possess different biologically active targets and have been studied for their potent anticancer [44], antimicrobial [45], anti-inflammatory [46] and antimalarial activities [47]. The efficacy of these drugs can be credited to their DNA-interacting capabilities.…”

Section: Coppermentioning

confidence: 99%

New Antimicrobial Strategies Based on Metal Complexes

2020

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Traditional organic antimicrobials mainly act on specific biochemical processes such as replication, transcription and translation. However, the emergence and wide spread of microbial resistance is a growing threat for human beings. Therefore, it is highly necessary to design strategies for the development of new drugs in order to target multiple cellular processes that should improve their efficiency against several microorganisms, including bacteria, viruses or fungi. The present review is focused on recent advances and findings of new antimicrobial strategies based on metal complexes. Recent studies indicate that some metal ions cause different types of damages to microbial cells as a result of membrane degradation, protein dysfunction and oxidative stress. These unique modes of action, combined with the wide range of three-dimensional geometries that metal complexes can adopt, make them suitable for the development of new antimicrobial drugs.

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“…They possess antioxidant (Grozav et al, 2017) and anti-Trypanosoma cruzi (da Silva et al, 2017) activities and are used as anti-prostate cancer agents (Saravanan et al, 2017). In view of the above importance of thiazole derivatives, we have undertaken the single-crystal X-ray diffraction study of the title compound, and the results are presented herein.…”

Section: Structure Descriptionmentioning

confidence: 99%