α-Aroylketene Dithioacetal Mediated Synthesis of (E)-3-(benzo[d]thiazol-2-ylamino)-2-(1-methyl-1H-indole-3-carbonyl)-3-(methylthio)acrylonitrile Derivatives and their Biological Evaluation

Bhale, Pravin S.; Chavan, Hemant V.; Dongare, Sakharam B.; Sankpal, Sagar T.; Bandgar, B. P.

doi:10.2174/1871520617666170912124258

Cited by 3 publications

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“…Acrylonitrile compounds are easily linked to aromatic rings, heterocycles and other structures, resulting in many new compounds. Acrylonitrile compounds are an effective antimalarial drug with good antioxidant and anti‐inflammatory properties 1 . Studies have shown that some derivatives have anti‐proliferative effects on U937, K562, Jurkat, and HeLa Tumor cells and are effective inducers of tumor cell apoptosis 2,3 .…”

Section: Introductionmentioning

confidence: 99%

The role of chlorine atom on the binding between acrylonitrile derivatives and fat mass and obesity‐associated protein

Bai

Gan

et al. 2020

J of Molecular Recognition

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In this work, seven acrylonitrile derivatives were selected as potential inhibitors of fat and obesity‐related proteins (FTO) by the aid of fluorescence spectroscopy, ultraviolet visible spectroscopy, molecular docking, and cytotoxicity methods. Results show that the interaction between 3‐amino‐2‐(4‐chlorophenyl)‐3‐phenylacrylonitrile (1a) and FTO was the strongest among these derivatives. Thermodynamic analysis and molecular modeling show that the main force between 1a and FTO is hydrophobic interaction. The cytotoxicity test showed that the IC50 value of 1a was 46.64 μmol/L, which indicated 1a had the smallest IC50 value and had the best inhibitory effect on the proliferation of leukemia K562 cells among the seven derivatives. Both our previous results and this work show that chlorine atoms play important role in the binding of small molecules and FTO. This work brings new information for the study of FTO inhibitors.

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Section: Introductionmentioning

confidence: 99%

The role of chlorine atom on the binding between acrylonitrile derivatives and fat mass and obesity‐associated protein

Bai

Gan

et al. 2020

J of Molecular Recognition

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Synthesis, characterization and biological evaluation of N- substituted indolyl chalcones as anticancer, anti-inflammatory and antioxidant agents

Chavan¹,

Ganapure²,

Mali

et al. 2023

Materials Today: Proceedings

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Ketene dithioacetal mediated synthesis of 1,3,4,5-tetrasubstituted pyrazole derivatives and their biological evaluation

Bhale

Bandgar

Dongare

et al. 2019

Phosphorus, Sulfur, and Silicon and the Related Elements

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α-Aroylketene Dithioacetal Mediated Synthesis of (E)-3-(benzo[d]thiazol-2-ylamino)-2-(1-methyl-1H-indole-3-carbonyl)-3-(methylthio)acrylonitrile Derivatives and their Biological Evaluation

Abstract: Among the compounds synthesized some of the compounds possess significant anticancer, antioxidant and anti-inflammatory properties.

Cited by 3 publications

References 0 publications

The role of chlorine atom on the binding between acrylonitrile derivatives and fat mass and obesity‐associated protein

The role of chlorine atom on the binding between acrylonitrile derivatives and fat mass and obesity‐associated protein

Synthesis, characterization and biological evaluation of N- substituted indolyl chalcones as anticancer, anti-inflammatory and antioxidant agents

Ketene dithioacetal mediated synthesis of 1,3,4,5-tetrasubstituted pyrazole derivatives and their biological evaluation

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