Synthesis and anticancer activity study of some new nitrogenous heterocycles / Hossam Hammouda Nada Hammouda ; Supervised Fadi Mohsen Awadallah , Walaa Ramadan Mahmoud

Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

Indole scaffold is an interesting ring system constituting the core of many compounds possessing a wide range of biological activities including anticancer, antibacterial, anti-inflammatory, antihypertensive, antiviral, anticonvulsant and antioxidant activity. Herein, we highlighted on the anticancer activity of the indole nucleus. The present investigation deals with the design and synthesis of three new series of indoles incorporating different sulfonamide moieties via different spacers namely, imine (IIIa-f), thiazolinone (VIIa-f) and imidazolinone spacers (Xa-l). The indole derivatives are considered as bioisosteres of the earlier compounds featuring a chromone nucleus which were very promising as carbonic anhydrase inhibitors. So, in continuation of the previous work, the new indole-sulphonamide hybrids were screened for their carbonic anhydrase inhibitory activity, cytotoxicity against colon HCT116 cell line and apoptotic effect. In silico pharmacokinetic profile study was also performed

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