Abstract
A series of novel 4H-benzo[h]chromenes 4, 6–11, 13, 14; 7H-benzo[h]chromeno[2,3-d]pyrimidines 15–18, 20, and 14H-benzo[h]chromeno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives 19a–e, 24 was prepared. The structures of the synthesized compounds were characterized on the basis of their spectral data. Some of the target compounds were examined for their antiproliferative activity against three cell lines; breast carcinoma (MCF-7), human colon carcinoma (HCT-116) and hepatocellular carcinoma (HepG-2). The cytotoxic behavior has been tested using MTT assay and the inhibitory activity was referenced to three standard anticancer drugs: vinblastine, colchicine and doxorubicin. The bioassays demonstrated that some of the new compounds exerted remarkable inhibitory effects as compared to the standard drugs on the growth of the three tested human tumor cell lines. The structure–activity relationships (SAR) study highlights that the antitumor activity of the target compounds was significantly affected by the lipophilicity of the substituent at 2- or 3- and fused rings at the 2,3-positions.
Highlights
In cancer research, multidrug resistance (MDR) is one of the major aspects that causes failure in therapeutic treatment
Some of the target compounds were examined for their antitumor activities in comparison to the standard drugs target compounds were examined for their antitumor activities in comparison to the standard drugs vinblastine, colchicine and doxorubicin
The synthesis of new compounds with potential applications as drug replacements is an area of high interest in literature in order to overcome the drug resistance issue
Summary
Multidrug resistance (MDR) is one of the major aspects that causes failure in therapeutic treatment This phenomenon could occur either via inherited or acquired approaches, which refers to the initial resistance to a specific drug and the development of resistance after successful treatment, respectively. Multicomponent reactions are some of the most some of the most successful procedures to prepare this class of molecules in good yields. Some of the most successful procedures to prepare this class of molecules in good yields. Successful proceduresorganic to prepare this class of molecules in good yields. Crolibulin (A) is currently in Phase I/II clinical trials for the treatment antitumor activity. 2-amino-4H-chromenes with with diverse diverse biological and pharmacological activities.
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