التفاصيل البيبلوغرافية
| العنوان: |
New Approaches for the Synthesis of Heterocyclic Compounds Derived from Cyclohexan-1,3-dione with Anti-proliferative Activities. |
| المؤلفون: |
Mohareb, Rafat Milad1 raafat_mohareb@yahoo.com, Milad, Yara Raafat2,3, Masoud, Ayat Ali1 |
| المصدر: |
Acta Chimica Slovenica. 2021, Vol. 68 Issue 1, p72-87. 16p. |
| مصطلحات موضوعية: |
*HETEROCYCLIC compounds synthesis, *HETEROCYCLIC compounds, *CHEMICAL synthesis, *OXIME derivatives, *HYDROXYLAMINE hydrochloride, *PYRAN derivatives, *HYDRAZINE derivatives |
| الملخص (بالإنجليزية): |
In the present work a series of heterocyclization reactions were adopted using cyclohexan-1,3-dione through its reaction with either furan-2-carbaldehyde or thiophene-2-carbaldehyde to give the corresponding ylidene derivatives 3a,b. The latter compounds underwent heterocyclization reactions to give thiophene and pyran derivatives 5a--d and 6a--d, respectively. Moreover, compounds 3a,b reacted with elemental sulfur and phenyl isothiocyanate to give the fused thiazole derivatives 8a,b. In addition, the reaction with either of hydrazine hydrate or phenylhydrazine has given the 4-hydrazono- 4,5,6,7-tetrahydro-2H-indazole derivatives 10a--d, respectively. Similarly, the reaction of either 3a or 3b with hydroxylamine hydrochloride gave the 6,7-dihydrobenzo[c]isoxazol-4(5H)-one oxime derivatives 12a and 12b, respectively. Other fused heterocyclic compounds were produced and their structures were elucidated. Evaluation of the synthesized compounds against selected cancer cell lines was performed. The most active compounds were further evaluated against tyrosine kinases and Pim-1 kinase inhibitions. [ABSTRACT FROM AUTHOR] |
| Abstract (Slovenian): |
V prispevku opisujemo serijo heterociklizacijskih reakcij, ki smo jih izvedli na cikloheksan-1,3-dionu s furan-2-karbaldehidom ali tiofen-2-karbaldehidom pri čemer sta nastala ustrezna ilidenska derivata 3a,b; ti dve spojini sta bili izhodišče za nadaljnje heterociklizacijske reakcije, ki so vodile do tiofenskih in piranskih derivatov 5a--d oz. 6a--d. Ob reakciji spojin 3a,b z elementarnim žveplom in fenil izotiocianatom sta nastala pripojena tiazolska derivata 8a,b. Pri reakciji s hidrazin hidratom ali fenilhidrazinom pa so nastali 4-hidrazono-4,5,6,7-tetrahidro-2H-indazolski derivati 10a--d. Podobno sta pri reakciji med 3a ali 3b s hidroksilamin hidrokloridom nastala 6,7-dihidrobenzo[c]izoksazol-4(5H)-on oksima 12a in 12b. Pripravili smo še več drugih heterocikličnih spojin in določili njihove strukture. Pripravljenim spojinam smo določili citotoksične aktivnosti na izbrane celične linije raka. Za najbolj aktivne spojine smo v nadaljevanju določili še inhibitorne lastnosti proti tirozin kinazam in Pim-1 kinazi. [ABSTRACT FROM AUTHOR] |
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