818375-08-5Relevant academic research and scientific papers
Synthesis, antitumor activity, and mechanism of action of benzo[a]pyrano[3,2-h]acridin-7-one analogues of acronycine
Nguyen, Tuan Minh,Sittisombut, Chavalit,Boutefnouchet, Sabrina,Lallemand, Marie-Christine,Michel, Sylvie,Koch, Michel,Tillequin, Fran?ois,Mazinghien, Romain,Lansiaux, Amélie,David-Cordonnier, Marie-Hélène,Pfeiffer, Bruno,Kraus-Berthier, Laurence,Léonce, Stéphane,Pierré, Alain
, p. 3383 - 3394 (2006)
Twenty-two derivatives belonging to the cis-1,2-diacyloxy-6-methoxy-3,3,14- trimethyl-1,2,3,14-tetrahydro-7H-benzo[a]pyrano[3,2-h]acridin-7-one series were synthesized in nine steps starting from 3,5-dimethoxy-acetanilide (5) and 2-methoxy-1-naphthalenecarboxylic acid (7). Most of them exhibited submicromolar cytotoxicity when tested against murine leukemia (L1210) and human epidermoid carcinoma (KB-3-1) cell lines. The cytotoxic activity correlated strongly with the ability of the compounds to form covalent adducts with purified DNA. Among the most active compounds, 25, with IC50 values of 0.7 and 0.15 μM against L1210 and KB-3-1, respectively, was selected for evaluation in vivo against Colon 38 adenocarcinoma implanted in mice. This compound was active at 3 mg/kg iv (day 12 and 24) with 3/7 tumor free mice by day 80.
Benzo[a]pyrano[3,2-h]acridin-7-one compounds
-
Page/Page column 18, (2010/02/10)
A compound selected from those of formula (I): 1 wherein: X and Y represent a group selected from hydrogen, halogen, hydroxy, alkoxy, nitro, cyano, alkyl, trihaloalkyl and NRaRb, wherein Ra and Rb are as defined in the description R1 represents hydrogen or alkyl R2 represents a group selected from hydrogen, alkyl, —OR″a, —NR′aR′b, -Ta-O″a, —N″a-Ta-NR′aR′b, —N″a—C(O)-TaH, —O—C(O) TaH, Ta-NR′aR′b, —NR″a-Ta-OR″a, —NR″a-Ta-CO2R″a and —N″a—C(O)-Ta-NR′aR′b, wherein R′a, R″a, R′b and Ta are as defined in the description R3 and R4 represent hydrogen or alkyl A represents a group of formula —CH(R5)CH(R6), —CH=C(R7)—, —C(R7)=CH—, —C(O)CH(R8) or —CH(R8)—C(O), wherein R5, R6, R7 and R8 are as defined in the description its isomers, N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.
