| Autor: |
Ryad N; Pharmaceutical Organic Chemistry Department, College of Pharmaceutical Sciences & Drug Manufacturing, Misr University for Science & Technology, 6th of October City, Giza, Egypt., Elmaaty AA; Medicinal Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said, 42526, Egypt., M Ibrahim I; Department of Clinical Pharmacology, Faculty of Medicine, King Abdulaziz University, Jeddah, Saudi Arabia., Ahmed Maghrabi AH; Department of Biology, Faculty of Applied Science, Umm Al-Qura University, Makkah, 24381, Saudi Arabia., Yahya Alahdal MA; Department of Biology, Faculty of Applied Science, Umm Al-Qura University, Makkah, 24381, Saudi Arabia., Saleem RM; Department of Laboratory Medicine, Faculty of Applied Medical Sciences, Al-Baha University, Al-Baha, 65431, Saudi Arabia., Zaki I; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said, 42526, Egypt., Ghany LMAA; Pharmaceutical Chemistry Department, College of Pharmaceutical Sciences & Drug Manufacturing, Misr University for Science & Technology, 6th of October City, Egypt. |
| Abstrakt: |
Aim: Using molecular hybridization approach, novel 18 quinoline derivatives ( 6a-11 ) were designed and synthesized as EGFR-TK inhibitors. Materials & methods: The antiproliferative activity was assessed against breast (MCF-7), leukemia (HL-60) and lung (A549) cancer cell lines. Moreover, the most active quinoline derivatives ( 6d and 8b ) were further investigated for their potential as EGFR-TK inhibitors. In addition, cell cycle analysis and apoptosis induction activity were conducted. Results: A considerable cytotoxic activity was attained with IC 50 values spanning from 0.06 to 1.12 μM. Besides, the quinoline derivatives 6d and 8b displayed potent inhibitory activity against EFGR with IC 50 values of 0.18 and 0.08 μM, respectively. Conclusion: Accordingly, the afforded quinoline derivatives can be used as promising lead anticancer candidates for future optimization. |
