Title:Synthesis and Antiproliferative Evaluation of Hybrids of Indolin-2-one and Quinazoline-4(3H)-one Linked via Imine Bond
Volume: 10
Issue: 1
Author(s): Wei-Yao Wu, Sheng-Li Cao, Bei-Bei Mao, Ji Liao, Zhong-Feng Li, Hao-Bin Song and Xingzhi Xu
Affiliation:
Keywords:
Antitproliferative activity, Hybrid, Indolin-2-one, Quinazolin-4(3H)-one, Synthesis, gastrointestinal stromal tumor, Nolatrexed, 2-Methylquinazolin, nitroquinazolin, MTT Assay
Abstract: A novel series of hybrids of indolin-2-one and quinazolin-4(3H)-one linked via an imine bond were
synthesized and tested for their inhibitory activity against the proliferation of a panel of five human cancer cell lines. We
found that compound 5c bearing 5-bromo substituent at the indolin-2-one ring exhibited weak cytotoxic activity with
percentages of inhibition ranging from 27% to 49% at 20 μM, while its counterpart 7c having 4-methoxybenzyl group at
the N1-position of indolin-2-one ring was more active with percentages of inhibition in range of 32-63%. These results
indicate that the presence of a bromo substituent at the 5-position and a 4-methoxybenzyl group at the N1-position of
indolin-2-one ring is important for the cytotoxic activity.
