New benzo[g]isoquinoline-5,10-diones and dihydrothieno [2,3-b]naphtho-4,9-dione derivatives

Synthesis of new pyrido[4,3- g and 3,4- g]quinoline-9,10-dione and dihydrothieno[2,3- g and 3,2-g]quinoline-4,9-dione derivatives and preliminary evaluation of cytotoxic activity

“…In fact, the regioisomers 4 and 5 showed similar activity at submicromolar concentration (Table 2) and were 4 time more potent that the carbocyclic analogue, (DTNQ, CC 50 = 1.2 µM). 7 The incorporation in DTQQs of 2-iodo or 3-fluorobenzoyl residues (6-9) conserved practically the activity in the same range, whereas the incorporation of Phe residues (10, 11) significantly reduced the cytotoxicity by 10 and 100 fold, respectively. This activity was recovered with derivatives supporting of phenylthio carbamoyl moiety (12, 13).…”

Synthesis of 2,3-dihydronaphtho[2,3-d][1,3]thiazole-4,9-diones and 2,3-dihydroanthra[2,3-d][1,3]thiazole-4,11-diones and novel ring contraction and fusion reaction of 3H-spiro[1,3-thiazole-2,1'-cyclohexanes] into 2,3,4,5-tetrahydro-1H-carbazole-6,11-diones

“…Meanwhile, in terms of further structural and chemical system modifications, the introduction of other heteroatoms (e.g., sulfur) through the heterocyclic ring incorporation to the quinone system has been one of the most interesting modifications. In fact, 2-alkylthio-1,4-naphthoquinones were found to show cell-growth inhibitory properties [2], and dihydrothienonaphthoquinones appeared to be potent antitumour compounds [3]. …”

Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams

“…Number of semi-synthetic derivatives like vinblastine [8], doxorubicin A [9], fluoroindolo carbazoles [10], certain derivatives of quinoline [11] have also been reported as therapeutic agents for the treatment of symptomatic BPH. Various synthetic derivatives of suberoylanilide hydroxamic acid [12], 2-arylthiazolidine-4-carboxylic acids [13] etc.…”