Synthesis and biological evaluation of thiazole and thiadiazole derivatives as potential anticancer agents
| Autor: | Sedanur Ekrek, Sevil Şenkardeş, Ömer Erdoğan, Özge Çevik |
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| Přispěvatelé: | Ekrek S., ŞENKARDEŞ S., ERDOĞAN Ö., ÇEVİK Ö. |
| Rok vydání: | 2022 |
| Předmět: |
STRUCTURAL-CHARACTERIZATION
1 3 4-THIADIAZOLE Kimya (çeşitli) Temel Bilimler (SCI) INHIBITION thiadiazole Organik Kimya Biochemistry Kimya Anticancer activity Inorganic Chemistry thiosemicarbazone KİMYA İNORGANİK VE NÜKLEER CHEMISTRY HYBRIDS Biyokimya KİMYA ORGANİK Biyoinorganik Kimya İnorganik Kimya CHEMISTRY INORGANIC & NUCLEAR Bioinorganic Chemistry Temel Bilimler Organic Chemistry apoptosis CHEMISTRY ORGANIC General Chemistry CANCER Genel Kimya Fizik Bilimleri Chemistry (miscellaneous) BAX Natural Sciences (SCI) Physical Sciences Natural Sciences thiazole |
| Zdroj: | Phosphorus, Sulfur, and Silicon and the Related Elements. 198:223-231 |
| ISSN: | 1563-5325 1042-6507 |
| DOI: | 10.1080/10426507.2022.2136665 |
| Popis: | A new series of 4-methyl-2-{2-[(aryl)methylidene]hydrazinyl}-1,3-thiazole (2a-i), N-(4-acetyl-5-aryl)4,5-dihydro-1,3,4-thiadiazol-2-yl)acetamides (3a-b) and N-(5-(4-(substituted phenyl)-1,3,4-thiadiazol-2-yl)acetamides (3c-i) were synthesized by the reaction of 2-((aryl)methylene)hydrazine-1-carbothioamides (1a-i) and acetic anhydride or chloroacetone. The cytotoxic activities of the products were evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay against Hela cervical cancer, MCF-7 breast carcinoma and HT-29 colorectal cancer cell lines. Thiazole based compounds 2a, 2b, 2f and 2i, bearing 4-bromothiophen-2-yl, naphthalen-2-yl, 2,5-difluorophenyl and 4-(trifluoromethoxy)phenyl moieties, respectively; also N-(4-acetyl-5-(naphthalen-2-yl)-4,5-dihydro-1,3,4-thiadiazol-2-yl)acetamide (3b) and N-(5-(2,6-difluorophenyl)-1,3,4-thiadiazol-2-yl)acetamide (3d) exhibited significant anticancer activity against three cancer cell lines. Moreover, these active compounds were further evaluated by apoptotic protein levels. The results showed that these thiazole and thiadiazole compounds induced apoptosis of cancer cells. |
| Databáze: | OpenAIRE |
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