Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1-yl)Acetophenone

Bedriye Seda Kurşun Aktar; Abdulraheem Mustafa Alkarabash; Ayşe Şahin Yağlıoğlu; Emine Elçin Oruç-emre

Makale detayları

Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1-yl)Acetophenone

Yazarlar:

Bedriye Seda Kurşun Aktar | Abdulraheem Mustafa Alkarabash | Ayşe Şahin Yağlıoğlu | Emine Elçin Oruç-emre

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Biochemistry and Cell Biology (Other) | Physical Chemistry (Other)

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry Vol.10 Issue 3, pp.861-868

Belge Tipi:

Makale

Yayın Tarihi:

8/2023

Belge Dili:

İngilizce

Document ID (Org No.):

2001292801

pISSN:

2149-0120

Anahtar kelimeler:

Özet:

 In this study, the synthesis of chalcone compounds 1-11 derived from 4-imidazol-1-ylacetophenone and the structure determination of these compounds by various spectroscopic methods were carried out. The anticancer activities of compounds 1-11 were examined against HeLa and PC-3 cancer cells at four different concentrations 100, 50, 25, and 5 µM using the BrdU ELISA assay. It was determined that all molecules except compounds 1 and 6 in HeLa cancer cells and compounds 2 and 8 against PC-3 cancer cells were more active against HeLa and PC-3 than the standard drug 5-fluorouracil 5-FU. The best activity against PC-3 cancer cells was compound 4 IC50: 1.390.00 µM. In addition, compound 11 IC50: 1.580.01 µM was found to have the highest activity against HeLa cancer cells. Compound 4 against PC-3 cancer cell and compound 11 against HeLa cancer cell displayed cell selective activity. The ADME properties and drug similarities of the molecules 1-11 using the SwissADME software were investigated. According to these properties, compounds 1-11 were found to obey Lipinski rules.

 In this study, the synthesis of chalcone compounds 1-11 derived from 4-imidazol-1-ylacetophenone and the structure determination of these compounds by various spectroscopic methods were carried out. The anticancer activities of compounds 1-11 were examined against HeLa and PC-3 cancer cells at four different concentrations 100, 50, 25, and 5 µM using the BrdU ELISA assay. It was determined that all molecules except compounds 1 and 6 in HeLa cancer cells and compounds 2 and 8 against PC-3 cancer cells were more active against HeLa and PC-3 than the standard drug 5-fluorouracil 5-FU. The best activity against PC-3 cancer cells was compound 4 IC50: 1.390.00 µM. In addition, compound 11 IC50: 1.580.01 µM was found to have the highest activity against HeLa cancer cells. Compound 4 against PC-3 cancer cell and compound 11 against HeLa cancer cell displayed cell selective activity. The ADME properties and drug similarities of the molecules 1-11 using the SwissADME software were investigated. According to these properties, compounds 1-11 were found to obey Lipinski rules.

 In this study, the synthesis of chalcone compounds 1-11 derived from 4-imidazol-1-ylacetophenone and the structure determination of these compounds by various spectroscopic methods were carried out. The anticancer activities of compounds 1-11 were examined against HeLa and PC-3 cancer cells at four different concentrations 100, 50, 25, and 5 µM using the BrdU ELISA assay. It was determined that all molecules except compounds 1 and 6 in HeLa cancer cells and compounds 2 and 8 against PC-3 cancer cells were more active against HeLa and PC-3 than the standard drug 5-fluorouracil 5-FU. The best activity against PC-3 cancer cells was compound 4 IC50: 1.390.00 µM. In addition, compound 11 IC50: 1.580.01 µM was found to have the highest activity against HeLa cancer cells. Compound 4 against PC-3 cancer cell and compound 11 against HeLa cancer cell displayed cell selective activity. The ADME properties and drug similarities of the molecules 1-11 using the SwissADME software were investigated. According to these properties, compounds 1-11 were found to obey Lipinski rules.

 In this study, the synthesis of chalcone compounds 1-11 derived from 4-imidazol-1-ylacetophenone and the structure determination of these compounds by various spectroscopic methods were carried out. The anticancer activities of compounds 1-11 were examined against HeLa and PC-3 cancer cells at four different concentrations 100, 50, 25, and 5 µM using the BrdU ELISA assay. It was determined that all molecules except compounds 1 and 6 in HeLa cancer cells and compounds 2 and 8 against PC-3 cancer cells were more active against HeLa and PC-3 than the standard drug 5-fluorouracil 5-FU. The best activity against PC-3 cancer cells was compound 4 IC50: 1.390.00 µM. In addition, compound 11 IC50: 1.580.01 µM was found to have the highest activity against HeLa cancer cells. Compound 4 against PC-3 cancer cell and compound 11 against HeLa cancer cell displayed cell selective activity. The ADME properties and drug similarities of the molecules 1-11 using the SwissADME software were investigated. According to these properties, compounds 1-11 were found to obey Lipinski rules.

Makale detayları

Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1-yl)Acetophenone

Yazarlar:

Bedriye Seda Kurşun Aktar | Abdulraheem Mustafa Alkarabash | Ayşe Şahin Yağlıoğlu | Emine Elçin Oruç-emre

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Biochemistry and Cell Biology (Other) | Physical Chemistry (Other)

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry Vol.10 Issue 3, pp.861-868

Belge Tipi:

Makale

Yayın Tarihi:

8/2023

Belge Dili:

İngilizce

Document ID (Org No.):

2001292801

pISSN:

2149-0120

ADME

antiproliferative activity

HeLa cell line

in silico.

PC-3 cell line

Sayı

Makale detayları

Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1-yl)Acetophenone

Yazarlar: Bedriye Seda Kurşun Aktar | Abdulraheem Mustafa Alkarabash | Ayşe Şahin Yağlıoğlu | Emine Elçin Oruç-emre

Yayıncı: Turkish Chemical Society

Ana Başlıklar: Biochemistry and Cell Biology (Other) | Physical Chemistry (Other)

Dergi: Journal of the Turkish Chemical Society Section A: Chemistry Vol.10 Issue 3, pp.861-868

Belge Tipi: Makale

Yayın Tarihi: 8/2023

Belge Dili: İngilizce

Document ID (Org No.): 2001292801

pISSN: 2149-0120

ADME

antiproliferative activity

HeLa cell line

in silico.

PC-3 cell line

Sayı

Yazarlar:

Bedriye Seda Kurşun Aktar | Abdulraheem Mustafa Alkarabash | Ayşe Şahin Yağlıoğlu | Emine Elçin Oruç-emre

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Biochemistry and Cell Biology (Other) | Physical Chemistry (Other)

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry Vol.10 Issue 3, pp.861-868

Belge Tipi:

Makale

Yayın Tarihi:

8/2023

Belge Dili:

İngilizce

Document ID (Org No.):

2001292801

pISSN:

2149-0120