Structural studies on bioactive compounds. 23. Synthesis of polyhydroxylated 2-phenylbenzothiazoles and a comparison of their cytotoxicities and pharmacological …

…, P Alexander, A Richter, DE Davies

Index: Stevens, Malcolm F. G.; McCall, Carol J.; Lelieveld, Peter; Alexander, Peter; Richter, Audrey; Davies, Donna E. Journal of Medicinal Chemistry, 1994 , vol. 37, # 11 p. 1689 - 1695

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Citation Number: 98

Abstract

A series of polyhydroxylated 2-phenylbenzothiazoles 3 has been prepared by demethylation of the precursor methoxylated 2-phenylbenzothiazoles 9. The key step in the construction of the benzothiazole nucleus involves a Jacobson cyclization of methoxylated thiobenzanilides 8. The target compounds inhibit WiDr human colon tumor cells and MCF-7 human mammary tumor cells in vitro with IC50 values in the low micromolar range, but the activity against ...