Evaluation of novel synthesized thiazole derivatives as potential aromatase inhibitors against breast cancer
Background: 4-Methylacetophenone is used in the preparation of starting materials, 4-methylphenacyle bromide (2) and 4-methylacetophenone thiosemicarbazole (3). Results: Several novel 2,4-disubstituted-1,3-thiazole analogues were obtained via the treatment of starting materials with 4-methylphenacyl bromide, acetyl chloride, aromatic aldehydes and bromination providing thiazole derivatives 5-8 respectively. Conclusion: Compounds 5-8 were investigated for their cytotoxic activity on MCF-7 and normal breast cells. Active compounds were found and in contrast to staurosporine, compound 8 displayed the most potent cytotoxic action that showed a strong inhibitory effect (aromatase) and (protein tyrosine kinase) enzymes, proving that the novel thiazole derivatives promoted the effective anticancer drug candidates.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2024 |
|---|---|
| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - year:2024 |
|---|---|
| Enthalten in: |
Future medicinal chemistry - (2024) vom: 15. März |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Fayad, Eman [VerfasserIn] |
|---|
| Links: |
|---|
| Anmerkungen: |
Date Revised 15.03.2024 published: Print-Electronic Citation Status Publisher |
|---|
| doi: |
10.4155/fmc-2023-0323 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM369777093 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM369777093 | ||
| 003 | DE-627 | ||
| 005 | 20240315234811.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 240315s2024 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.4155/fmc-2023-0323 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1331.xml |
| 035 | |a (DE-627)NLM369777093 | ||
| 035 | |a (NLM)38488019 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Fayad, Eman |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Evaluation of novel synthesized thiazole derivatives as potential aromatase inhibitors against breast cancer |
| 264 | 1 | |c 2024 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Revised 15.03.2024 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status Publisher | ||
| 520 | |a Background: 4-Methylacetophenone is used in the preparation of starting materials, 4-methylphenacyle bromide (2) and 4-methylacetophenone thiosemicarbazole (3). Results: Several novel 2,4-disubstituted-1,3-thiazole analogues were obtained via the treatment of starting materials with 4-methylphenacyl bromide, acetyl chloride, aromatic aldehydes and bromination providing thiazole derivatives 5-8 respectively. Conclusion: Compounds 5-8 were investigated for their cytotoxic activity on MCF-7 and normal breast cells. Active compounds were found and in contrast to staurosporine, compound 8 displayed the most potent cytotoxic action that showed a strong inhibitory effect (aromatase) and (protein tyrosine kinase) enzymes, proving that the novel thiazole derivatives promoted the effective anticancer drug candidates | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a World Health Organization | |
| 650 | 4 | |a anti-breast cancer | |
| 650 | 4 | |a cell cycle analysis | |
| 650 | 4 | |a in vitro cytotoxic activity | |
| 650 | 4 | |a inhibitory effect PTK enzyme | |
| 650 | 4 | |a mass spectrometry | |
| 650 | 4 | |a molecular docking study | |
| 650 | 4 | |a normal cell lines | |
| 650 | 4 | |a potential aromatase inhibitors | |
| 650 | 4 | |a thiazole derivatives | |
| 700 | 1 | |a Binjawhar, Dalal Nasser |e verfasserin |4 aut | |
| 700 | 1 | |a Ageeli, Abeer A |e verfasserin |4 aut | |
| 700 | 1 | |a Alshaya, Dalal Sulaiman |e verfasserin |4 aut | |
| 700 | 1 | |a Elsaid, Fahmy Gad |e verfasserin |4 aut | |
| 700 | 1 | |a Mahmoud, Amr Yasser |e verfasserin |4 aut | |
| 700 | 1 | |a Radwan, Eman M |e verfasserin |4 aut | |
| 700 | 1 | |a Mahdy, Ahmed Re |e verfasserin |4 aut | |
| 700 | 1 | |a Elian Sophy, Mohamed Ahmed |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Future medicinal chemistry |d 2009 |g (2024) vom: 15. März |w (DE-627)NLM194822109 |x 1756-8927 |7 nnns |
| 773 | 1 | 8 | |g year:2024 |g day:15 |g month:03 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.4155/fmc-2023-0323 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |j 2024 |b 15 |c 03 | ||