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Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Anticancer Evaluation of Novel Quinazolinone Acetamides: Synthesis and Characterization
Farhana Hakim1, Roshan Salfi1, Darna Bhikshapathi2
1Department of Pharmaceutical Sciences, Career Point University, Kota, Rajasthan-325003, India.
Background:
According to the global cancer report 2019, the burden of cancer will exceed more than 18 million, becoming one of the major causes of global mortality rate. There is a pressing need to establish novel drug candidates for cancer treatment, though many anticancer agents are available in the market owing to their adverse effects. In recent years, quinazoline and its derivatives have been considered as a novel class of cancer chemotherapeutic agents that show promising activity against different tumors.
Objective:
To evaluate the anti-cancer potential of the novel class of quinazoline tethered acetamide derivatives against six different cancer cell lines.
Methods:
A novel series of various substituted quinazolinone acetamides were synthesized through a feasible scheme. The synthetic scheme involves the conversion of benzoxazinone (from anthranilic acid and benzoyl chloride) intermediate to 3-amino quinazoline-4-one which further converted to the final amide by tethering with the propionyl chloride employing Schotten-Baumann Reaction conditions. All the synthesized derivatives characterized by IR, 1HNMR and MASS spectral methods and anti-cancer activity were evaluated by employing MTT assay for six cancer cell lines and one normal human cell line.
Results:
All the synthesized compounds were screened for anti-cancer activity against six cancer cell lines, including A 549 (lung), DU 145 (prostate), HT 29 (colon), MCF-7 (breast), SiHA (cervical), B16F10 (mouse skin melanoma) and one normal human fibroblast cell lines. All the compounds displayed a decent cytotoxicity profile when compared with the standard drug doxorubicin. Among the synthesized compounds (5a to 5n) tested, two compounds, 5f and 5g have demonstrated excellent cytotoxicity against SiHA and MCF-7 cancer cell lines.
Conclusion:
Comparatively most of the compounds displayed decent cytotoxicity potential relative to the standard drug doxorubicin. Further investigations are needed to establish the detailed mechanism of action of the developed novel quinazolinone acetamides.
Insights
Novel quinazolinone acetamides show promising anticancer activity against various cancer cell lines. Two derivatives, 5f and 5g, demonstrated excellent cytotoxicity, offering potential new chemotherapeutic agents.
Area of Science:
- Medicinal Chemistry
- Oncology
- Drug Discovery
Background:
- Cancer represents a significant global health burden, necessitating novel therapeutic strategies.
- Existing chemotherapeutic agents often have adverse effects, driving the search for new drug candidates.
- Quinazoline derivatives have emerged as a promising class of anticancer agents with potential against various tumors.
Purpose of the Study:
- To synthesize and evaluate the anticancer potential of novel quinazoline tethered acetamide derivatives.
- To assess the cytotoxicity of these compounds against a panel of human cancer cell lines.
Main Methods:
- A series of substituted quinazolinone acetamides were synthesized.
- Compounds were characterized using IR, 1HNMR, and MASS spectral methods.
- Anticancer activity was evaluated using the MTT assay against six cancer cell lines and one normal cell line.
Main Results:
- All synthesized compounds exhibited cytotoxicity against tested cancer cell lines, comparable to the standard drug doxorubicin.
- Compounds 5f and 5g displayed significant cytotoxicity against SiHA (cervical) and MCF-7 (breast) cancer cell lines.
- The novel derivatives showed a decent cytotoxicity profile against lung, prostate, colon, and melanoma cancer cells.
Conclusions:
- The synthesized quinazolinone acetamides possess significant anticancer potential.
- Compounds 5f and 5g are identified as lead candidates for further investigation.
- Further studies are required to elucidate the detailed mechanism of action of these novel agents.
