<jats:title>3</jats:title> <jats:p>Phytochemical investigations of Calotropis procera leaves have led to the isolation of two new compounds: quercetagetin-6-methyl ether 3-O-β-D-<jats:sup>4</jats:sup>C<jats:sub>1</jats:sub>-galacturonopyranoside () and (E)-3-(4-methoxyphenyl-2-O-β-D-<jats:sup>4</jats:sup>C<jats:sub>1</jats:sub>-glucopyranoside)-methyl propenoate (<jats:bold>4</jats:bold>), along with eleven known metabolites: nine flavonol and two cinnamic acid derivatives. All metabolites were isolated for the first time from the genus Calotropis, except for <jats:bold>1 </jats:bold>isolated previously from Calotropis gigantea. The structures were determined by spectroscopic methods (UV, ESI-MS, <jats:sup>1</jats:sup>H, <jats:sup>13</jats:sup>C NMR, <jats:sup>1</jats:sup>H-<jats:sup>1</jats:sup>H COSY, HSQC, and HMBC). The radical scavenging activity of the aqueous methanol extract and compounds <jats:bold>8 </jats:bold>- <jats:bold>13 </jats:bold>was measured by the 1,1-diphenyl- 2-picrylhydrazyl (DPPH) method. Cytotoxic screening of the same compounds was carried out on brine shrimps as well