Abstract: The invention provides novel tyloindicines analogues and related processes, pharmaceutical compositions, and methods. The novel tyloindicines are useful in a wide variety of antiviral, antineoplastic, antibacterial, and anti-inflammatory applications. Preferred embodiments of the instant invention include the novel tyloindicine designated herein as compound IT-3 (NSC-716802). Compounds of the instant invention have exhibited potent antiviral and anticancer activity in vitro. The invention further provides novel methods of treating neoplastic, bacterial, viral, and anti-inflammatory disorders using tyloindicines including the novel tyloindicine analogues of the instant invention. The invention also provides novel syntheses of tyloindicines including the novel tyloindicines analogues of the instant invention.