<abstract xmlns="http://www.w3.org/1999/xhtml">A novel series of quinazoline derivatives <bold>2-8</bold>, <bold>10-12</bold> were designed and synthesized. Structures of the newly synthesized compounds were confirmed by elemental analyses, IR, 1H and 13C NMR spectral data. All the newly synthesized compounds were evaluated for <italic>in vitro</italic> cytotoxic activity against the breast cancer cell line MCF-7. Seven of the novel compounds exhibited higher activity than the reference drug doxorubicin. The corresponding compounds <bold>3</bold>, <bold>4</bold>, <bold>5</bold>, <bold>8</bold>, <bold>10</bold>, <bold>11</bold> and <bold>12</bold> exhibited higher activity with <italic>IC</italic>50 values from 22.75 to 43.44 μmol L−1, compared to the reference drug doxorubicin with <italic>IC</italic>50 value of 47.90 μmol L−1. Also, compounds <bold>1</bold>, <bold>6</bold>, and <bold>9</bold> are nearly as active as doxorubicin with <italic>IC</italic>50 values of 48.31, 48.90, and 48.91 μmol L−1, respectively, while compounds <bold>2</bold> and <bold>7</bold> exhibited a moderate activity with <italic>IC</italic>50 values of 50.44 and 52.37 μmol L−1. In addition, compound <bold>13</bold> showed no activity. Cytotoxic screening of the tested copmpounds offered an encouraging framework that may lead to the discovery of potent anti-breast cancer activity.</abstract>

A novel series of quinazoline derivatives 2-8, 10-12 were designed and synthesized. Structures of the newly synthesized compounds were confirmed by elemental analyses, IR, 1H and 13C NMR spectral data. All the newly synthesized compounds were evaluated for in vitro cytotoxic activity against the breast cancer cell line MCF-7. Seven of the novel compounds exhibited higher activity than the reference drug doxorubicin. The corresponding compounds 3, 4, 5, 8, 10, 11 and 12 exhibited higher activity with IC50 values from 22.75 to 43.44 μmol L−1, compared to the reference drug doxorubicin with IC50 value of 47.90 μmol L−1. Also, compounds 1, 6, and 9 are nearly as active as doxorubicin with IC50 values of 48.31, 48.90, and 48.91 μmol L−1, respectively, while compounds 2 and 7 exhibited a moderate activity with IC50 values of 50.44 and 52.37 μmol L−1. In addition, compound 13 showed no activity. Cytotoxic screening of the tested copmpounds offered an encouraging framework that may lead to the discovery of potent anti-breast cancer activity.

Novel 4-aminoquinazoline derivatives as new leads for anticancer drug discovery

Department of Pharmacognosy College of Pharmacy, King Saud University, Riyadh, P.O. 2457, Riyadh 11451, Saudi Arabia

Department of Drug Radiation Research, National Centre For Radiation Research and Technology Atomic Energy Authority, P.O. Box 29 Nasr City, Cairo, Egypt

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

{"article-title":"Novel 4-aminoquinazoline derivatives as new leads for anticancer drug discovery"}

A novel series of quinazoline derivatives 2-8, 10-12 were designed and synthesized. Structures of the newly synthesized compounds were confirmed by elemental...

Novel 4-aminoquinazoline derivatives as new leads for anticancer drug discovery

Publié en ligne: 30 sept. 2015

Pages: 299 - 309

Accepté: 16 févr. 2015

DOI: https://doi.org/10.1515/acph-2015-0021

Mots clés
4-aminoquinazoline derivatives, synthesis, anti-breast cancer activity

© Mostafa M. Ghorab et al.

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Novel 4-aminoquinazoline derivatives as new leads for anticancer drug discovery

Publié en ligne: 30 sept. 2015

Pages: 299 - 309

Accepté: 16 févr. 2015

DOI: https://doi.org/10.1515/acph-2015-0021

Mots clés4-aminoquinazoline derivatives, synthesis, anti-breast cancer activity

© Mostafa M. Ghorab et al.

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Mots clés
4-aminoquinazoline derivatives, synthesis, anti-breast cancer activity