Synthesis and Biological Evaluation of N-[2-(4-Hydroxyphenylamino)-pyridin-3-yl]-4-methoxy-benzenesulfonamide (ABT-751) Tricyclic Analogues as Antimitotic and …

…, P Berthelot, X Thuru, N Lebegue

Index: Lebegue, Nicolas; Gallet, Sebastien; Flouquet, Nathalie; Carato, Pascal; Pfeiffer, Bruno; Renard, Pierre; Leonce, Stephane; Pierre, Alain; Chavatte, Philippe; Berthelot, Pascal Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7363 - 7373

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Abstract

Benzopyridothiadiazepine (2a) and benzopyridooxathiazepine (2b) were modified to produce tricyclic quinazolinone 15–18 or benzothiadiazine 26–27 derivatives. These compounds were evaluated in cytotoxicity and tubulin inhibition assays and led to potent inhibitors of tubulin polymerization. N-[2 (4-Methoxyphenyl) ethyl]-1, 2-dihydro-pyrimidino [2, 1-b] quinazolin-6-one (16a) exhibited the best in vitro cytotoxic activity (GI50 10–66.9 nM) ...