Design, synthesis and in vitro antiproliferative activity of novel isatin-quinazoline hybrids
Fares, Mohamed; Eldehna, Wagdy M; Abou-Seri, Sahar M; Abdel-Aziz, Hatem A; Aly, Mohamed H; Tolba, Mai;
Abstract
Using a molecular hybridization approach, a new series of isatin-quinazoline hybrids 15a-o was designed and synthesized via two different synthetic routes. The target compounds 15a-o were prepared by the reaction of quinazoline hydrazines 12a-e with indoline-2,3-diones 13a-c or by treating 4-chloroquinazoline derivatives 11a-e with isatin hydrazones 14a-c. The in vitro anticancer activity of the newly synthesized hybrids was evaluated against the liver HepG2, breast MCF-7 and colon HT-29 cancer cell lines. A distinctive selective growth inhibitory effect was observed towards the HepG2 cancer cell line. Compounds 15b, 15g and 15l displayed the highest potency, with IC50 values ranging from 1.0 ± 0.2 to 2.4 ± 0.4 μM, and they were able to induce apoptosis in HepG2 cells, as evidenced by enhanced expression of the pro-apoptotic protein Bax and reduced expression of the anti-apoptotic protein Bcl-2, in addition to increased caspase-3 levels.
Other data
Title | Design, synthesis and in vitro antiproliferative activity of novel isatin-quinazoline hybrids | Authors | Fares, Mohamed; Eldehna, Wagdy M; Abou-Seri, Sahar M; Abdel-Aziz, Hatem A; Aly, Mohamed H; Tolba, Mai | Keywords | Antiproliferative activity; Isatins; Molecular hybridization; Quinazolines | Issue Date | Feb-2015 | Journal | Archiv der Pharmazie | ISSN | 0365-6233 1521-4184 |
DOI | 10.1002/ardp.201400337 | PubMed ID | 25664631 | Scopus ID | 2-s2.0-84922572823 |
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