Abstract
A novel series of 4-substituted amino-7,8-dimethoxy-1-phenylimidazo[1,5-a]quinazolin-5(4H)-one derivatives was designed, synthesized and tested for their antitumor activity against a human mammary carcinoma cell line (MCF7). Compound 5a was found to be the most active derivative. Physico-chemical parameters were also determined and revealed that most of the compounds obeyed the “rule of five” properties with good absorption percentages. 2D-QSAR studies revealed a well predictive and statistically significant and cross validated QSAR model that helps to explore some expectedly potent compounds.
Highlights
Struggling efforts for the treatment and eradication of cancer have grown tremendously in the last few years led to the decrease in cancer death rates by 1.8% per year in men and by 1.5% per year in women [1]
The control of disseminated tumor growth by systemically active chemotherapeutic agents remains a major challenge for cancer chemotherapy, despite decades of focused efforts
With methyl 2-amino-4,5-dimethoxybenzoate in glacial acetic acid in the presence of sodium acetate. This reaction proceeded through open intermediates which were recyclized in the presence of glacial acetic acid to afford the imidazolinones [28]
Summary
Struggling efforts for the treatment and eradication of cancer have grown tremendously in the last few years led to the decrease in cancer death rates by 1.8% per year in men and by 1.5% per year in women [1]. Cancer is characterized by a deregulation of the cell cycle, resulting in progressive loss of the cellular differentiation and non-controlled cellular growth [2,3]. The control of disseminated tumor growth by systemically active chemotherapeutic agents remains a major challenge for cancer chemotherapy, despite decades of focused efforts. A small bioactive molecule, is a prominent structural motif found in numerous biologically active compounds. Imidazolinones such as I [12] (Figure 1) and methoxyquinazoline
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