The use of β-diketone and cyanomethylene reagents for the synthesis of heterocyclic compounds and their fused derivatives with anti-tumor activities /
Hanan Maged Labib,
The use of β-diketone and cyanomethylene reagents for the synthesis of heterocyclic compounds and their fused derivatives with anti-tumor activities / استخدام كواشف البيتا ثنائى الكيتون وسيانوالمثيلين النشطة لتحضير مركبات غير متجانسة الحلقة ومشتاقاتها الملتحمة كمضادات للأورام النشطة / by Hanan Maged Labib ; Supervisors Prof. Dr. Rafat Milad Mohareb, Prof. Dr. Refaat Ibrahim Naseem. - 218 pages : illustrations ; 25 cm. + CD.
Thesis (Ph.D)-Cairo University, 2024.
Bibliography: pages 201-218.
In this thesis we worked on synthesizing new heterocyclic compounds using B-diketones and cyanomethylene reagents. The synthetic schemes involved multicomponent reactions. Gewald’s thiophene synthesis was also involved to produce biologically active fused thiophene compounds. Anti-proliferative evaluations and inhibitions for the new synthesized compounds and their fused derivatives towards selected cancer cell lines were carried out along with foretinib as the positive control. The results revealed that many of the new compounds have high inhibition. This opens the way for more research especially in the drugs synthesis field ﻓﻲ ھﺬه اﻟﺮﺳﺎﻟﺔ، ﻗﻤﻨﺎ ﺑﺘﺤﻀﯿﺮ ﻣﺮﻛﺒﺎت ﻏﯿﺮ ﻣﺘﺠﺎﻧﺴﺔ اﻟﺤﻠﻘﺔ ﺑﺎﺳﺘﺨﺪام اﻟﺒﯿﺘﺎ ﺛﻨﺎﺋﻲ اﻟﻜﯿﺘﻮن و اﻟﺴﯿﺎﻧﻮﻣﯿﺜﯿﻠﯿﻦ. ﺗﻀﻤﻨﺖ اﻟﻤﺨﻄﻄﺎت
ﺗﻔﺎﻋﻼت ﻣﺘﻌﺪدة اﻟﻤﻜﻮﻧﺎت.اﯾﻀﺎ ﺗﻢ اﺳﺘﺨﺪام ﺗﻔﺎﻋﻞ Gewald’s ﻟﺘﺤﻀﯿﺮ ﻣﺮﻛﺒﺎت اﻟﺜﯿﻮﻓﯿﻦ اﻟﻨﺸﻄﺔ. ﺗﻢ ﺗﻘﯿﯿﻢ اﻟﻨﺸﺎط اﻟﻤﻀﺎد ﻟﻠﺘﻜﺎﺛﺮ
و اﻟﺘﺜﺒﯿﻂ ﻟﻠﻤﺮﻛﺒﺎت اﻟﻤﺼﻨﻌﺔ ﺣﺪﯾﺜﺎ و ﻣﺸﺘﻘﺎﺗﮭﺎ ﻣﻘﺎﺑﻞ ﺧﻄﻮط اﻟﺨﻼﯾﺎ اﻟﺴﺮطﺎﻧﯿﺔ ﺟﻨﺒﺎ اﻟﻲ ﺟﻨﺐ ﻣﻊ foretinib ﻛﻌﻨﺼﺮ ﺗﺤﻜﻢ اﯾﺠﺎﺑﻲ. اظﮭﺮت اﻟﻨﺘﺎﺋﺞ ان اﻟﻤﺮﻛﺒﺎت ﻟﺪﯾﮭﺎ ﺗﺜﺒﯿﻂ ﻋﺎﻟﻲ. ھﺬا ﯾﻔﺘﺢ اﻟﻄﺮﯾﻖ ﻟﻤﺰﯾﺪ ﻣﻦ اﻟﺒﺤﺚ ﺧﺎﺻﺔ ﻓﻲ ﻣﺠﺎل ﺻﻨﺎﻋﺔ اﻟﺪواء
Text in English and abstract in Arabic & English.
Heterocyclic compounds
B-diketone Heterocyclic compounds cyanomethylene Gewald’s thiophene synthesis anti-tumor activity
547.59
The use of β-diketone and cyanomethylene reagents for the synthesis of heterocyclic compounds and their fused derivatives with anti-tumor activities / استخدام كواشف البيتا ثنائى الكيتون وسيانوالمثيلين النشطة لتحضير مركبات غير متجانسة الحلقة ومشتاقاتها الملتحمة كمضادات للأورام النشطة / by Hanan Maged Labib ; Supervisors Prof. Dr. Rafat Milad Mohareb, Prof. Dr. Refaat Ibrahim Naseem. - 218 pages : illustrations ; 25 cm. + CD.
Thesis (Ph.D)-Cairo University, 2024.
Bibliography: pages 201-218.
In this thesis we worked on synthesizing new heterocyclic compounds using B-diketones and cyanomethylene reagents. The synthetic schemes involved multicomponent reactions. Gewald’s thiophene synthesis was also involved to produce biologically active fused thiophene compounds. Anti-proliferative evaluations and inhibitions for the new synthesized compounds and their fused derivatives towards selected cancer cell lines were carried out along with foretinib as the positive control. The results revealed that many of the new compounds have high inhibition. This opens the way for more research especially in the drugs synthesis field ﻓﻲ ھﺬه اﻟﺮﺳﺎﻟﺔ، ﻗﻤﻨﺎ ﺑﺘﺤﻀﯿﺮ ﻣﺮﻛﺒﺎت ﻏﯿﺮ ﻣﺘﺠﺎﻧﺴﺔ اﻟﺤﻠﻘﺔ ﺑﺎﺳﺘﺨﺪام اﻟﺒﯿﺘﺎ ﺛﻨﺎﺋﻲ اﻟﻜﯿﺘﻮن و اﻟﺴﯿﺎﻧﻮﻣﯿﺜﯿﻠﯿﻦ. ﺗﻀﻤﻨﺖ اﻟﻤﺨﻄﻄﺎت
ﺗﻔﺎﻋﻼت ﻣﺘﻌﺪدة اﻟﻤﻜﻮﻧﺎت.اﯾﻀﺎ ﺗﻢ اﺳﺘﺨﺪام ﺗﻔﺎﻋﻞ Gewald’s ﻟﺘﺤﻀﯿﺮ ﻣﺮﻛﺒﺎت اﻟﺜﯿﻮﻓﯿﻦ اﻟﻨﺸﻄﺔ. ﺗﻢ ﺗﻘﯿﯿﻢ اﻟﻨﺸﺎط اﻟﻤﻀﺎد ﻟﻠﺘﻜﺎﺛﺮ
و اﻟﺘﺜﺒﯿﻂ ﻟﻠﻤﺮﻛﺒﺎت اﻟﻤﺼﻨﻌﺔ ﺣﺪﯾﺜﺎ و ﻣﺸﺘﻘﺎﺗﮭﺎ ﻣﻘﺎﺑﻞ ﺧﻄﻮط اﻟﺨﻼﯾﺎ اﻟﺴﺮطﺎﻧﯿﺔ ﺟﻨﺒﺎ اﻟﻲ ﺟﻨﺐ ﻣﻊ foretinib ﻛﻌﻨﺼﺮ ﺗﺤﻜﻢ اﯾﺠﺎﺑﻲ. اظﮭﺮت اﻟﻨﺘﺎﺋﺞ ان اﻟﻤﺮﻛﺒﺎت ﻟﺪﯾﮭﺎ ﺗﺜﺒﯿﻂ ﻋﺎﻟﻲ. ھﺬا ﯾﻔﺘﺢ اﻟﻄﺮﯾﻖ ﻟﻤﺰﯾﺪ ﻣﻦ اﻟﺒﺤﺚ ﺧﺎﺻﺔ ﻓﻲ ﻣﺠﺎل ﺻﻨﺎﻋﺔ اﻟﺪواء
Text in English and abstract in Arabic & English.
Heterocyclic compounds
B-diketone Heterocyclic compounds cyanomethylene Gewald’s thiophene synthesis anti-tumor activity
547.59