Novel heterocyclic analogs of resveratrol, (E)-stilbene analogs, were readily prepared by conjugation of a heterocyclic benzothiazolium moiety with the core styrene structure of resveratrol and evaluated for their biological properties. The results showed that these analogs were superior to resveratrol in 1) anti-angiogenesis in vitro, 2) nitric oxide inhibition in vitro, and 3) inhibition of carrageenan-induced edema in vivo. In summary, introduction of a heterocyclic benzothiazolium moiety to replace one of two aromatic rings from the core stilbene structure of resveratrol provided beneficial biological properties and is worthy of further investigation.