CYTOSTATIC ACTIVITY AGAINST HELA-CELLS OF A SERIES OF INDAZOLE AND INDOLE-DERIVATIVES - SYNTHESIS AND EVALUATION OF SOME ANALOGS

The remarkable cytostatic activity of 1-substituted indazolols 2a, b, condensed indazolinones 4a-c and indoxyl derivatives 5a, b against HeLa cells is reported. Three different approaches to the synthesis of indazolophthalazinone 4a, representing alternatives to those previously reported, were studied. Several compounds related to the mentioned indazolols and indazolinones were obtained and their cytostatic activity against HeLa cells was tested. Among them we can mention the tetracyclic SO2 analogue 14 and the condensed pyridine derivative 18, the tricyclic pyrazolophthalazinone 22 and the bicyclic pyrazolodiazepinone 25, which were prepared by taking advantage of the reactivity of heterocyclic spiro aminimides.