作者
Tarfah Al-Warhi, Mahmoud F Abo-Ashour, Hadia Almahli, Ohoud J Alotaibi, Mohammad M Al-Sanea, Ghada H Al-Ansary, Hanaa Y Ahmed, Mahmoud M Elaasser, Wagdy M Eldehna, Hatem A Abdel-Aziz
发表日期
2020/1/1
期刊
Journal of enzyme inhibition and medicinal chemistry
卷号
35
期号
1
页码范围
1300-1309
出版商
Taylor & Francis
简介
As a continuation for our previous work, a novel set of N-alkylindole-isatin conjugates (7, 8a–c, 9 and 10a–e) is here designed and synthesised with the prime aim to develop more efficient isatin-based antitumor candidates. Utilising the SAR outputs from the previous study, our design here is based on appending four alkyl groups with different length (ethyl and n-propyl), bulkiness (iso-propyl) and unsaturation (allyl) on N-1 of indole motif, with subsequent conjugation with different N-unsubstituted isatin moieties to furnish the target conjugates. As planned, the adopted strategy achieved a substantial improvement in the growth inhibitory profile for the target conjugates in comparison to the reported lead VI. The best results were obtained with N-propylindole –5-methylisatin hybrid 8a which displayed broad spectrum anti-proliferative action with efficient sub-panel GI50 (MG-MID) range from 1.33 to 4.23 µM, and …
引用总数
20202021202220232024313101713