Novel Benzopyridothiadiazepines as Potential Active Antitumor Agents

• Published in: Journal of medicinal chemistry Vol. 48; no. 23; pp. 7363 - 7373
• Main Authors: Lebegue, Nicolas, Gallet, Sebastien, Flouquet, Nathalie, Carato, Pascal, Pfeiffer, Bruno, Renard, Pierre, Léonce, Stéphane, Pierré, Alain, Chavatte, Philippe, Berthelot, Pascal
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 17.11.2005; Amer Chemical Soc
• Subjects: Aminophenols - chemistry; Animals; Antimitotic Agents - chemical synthesis; Antimitotic Agents - chemistry; Antimitotic Agents - pharmacology; Antineoplastic agents; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Biological and medical sciences; Cell Line, Tumor; Chemical Sciences; Chemistry, Medicinal; Cyclic S-Oxides - chemical synthesis; Cyclic S-Oxides - chemistry; Cyclic S-Oxides - pharmacology; Drug Screening Assays, Antitumor; General aspects; Heterocyclic Compounds, 3-Ring - chemical synthesis; Heterocyclic Compounds, 3-Ring - chemistry; Heterocyclic Compounds, 3-Ring - pharmacology; Life Sciences & Biomedicine; Medical sciences; Mice; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Science & Technology; Structure-Activity Relationship; Sulfonamides - chemical synthesis; Sulfonamides - chemistry; Sulfonamides - pharmacology; Thiazepines - chemical synthesis; Thiazepines - chemistry; Thiazepines - pharmacology; Tubulin Modulators - chemical synthesis; Tubulin Modulators - chemistry; Tubulin Modulators - pharmacology; IN-VITRO; COLCHICINE; INHIBITION; MICROTUBULES; GROWTH; TUBULIN POLYMERIZATION; SULFONAMIDE; DYNAMIC INSTABILITY; BINDING; ANTITUBULIN ACTIVITY; Antineoplastic agent; Leukemia; Rodentia; Antitubulin; In vitro; L1210 cell line; Vertebrata; Mammalia; Cell line; Sultam; Structure activity relation; Mouse; Chemical synthesis; Antimitotic; Tumor cell; Lipophilicity; Physicochemical properties

The synthesis of novel thiadiazepine derivatives, that could be considered as constraint analogues of E-7010, are reported. These molecules were evaluated for their antiproliferative activity toward the murine L1210 leukemia cell line. Flow cytometric studies performed on L1210 cells with the most c...