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Synthesis, cytotoxic activity and 2D-QSAR study of some imidazoquinazoline derivatives.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2014 Mar 24; Vol. 19 (3), pp. 3777-92. Date of Electronic Publication: 2014 Mar 24. - Publication Year :
- 2014
-
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.
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Cell Line, Tumor
Drug Screening Assays, Antitumor
Humans
MCF-7 Cells
Quinazolines chemical synthesis
Imidazoles chemistry
Quantitative Structure-Activity Relationship
Quinazolines chemistry
Quinazolines toxicity
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 19
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 24662088
- Full Text :
- https://doi.org/10.3390/molecules19033777