Synthesis and Cytotoxicity of Novel Hexahydrothienocycloheptapyridazinone Derivatives

Abstract

Designed as a new group of tricyclic molecules containing the thienocycloheptapyridazinone ring system, a number of 2N-substituted-hexahydrothieno-cycloheptapyridazinone derivatives were synthesized and their biological activity evaluated. Among the synthesized compounds, derivatives 7d and 7h were found to possess cytotoxic activity against non-small cell lung cancer and central nervous system cancer cell lines, respectively.

Multitarget‐Directed Tricyclic Pyridazinones as G Protein‐Coupled Receptor Ligands and Cholinesterase Inhibitors

“…[19] Compounds 24 [37] and 25 [36] were prepared as reported in the literature. RP-HPLC analyses were run on aZ ORBAX Eclipse Plus C 18 column (250 mm 4.6 mm ID, 5 mm) using aU V/Vis detector at 254 nm and 280 nm.…”

“…Tricyclic pyridazinone 1 [19] (Figure 2) wasu sed as ar eference platform for the production of al ibraryo fc ompounds bearing linear polymethylenec hains of different length joining the tricyclic scaffold and differently substituted cyclic amines. Ta rget compounds 2-7 were synthesized by the general route depicted in Scheme 1, starting from the halogen derivatives 8-13 (obtained by alkylation of pyridazinones 14 [35] with the appropriate alkyl dihalides)t hat were reacted with the appropriate heterocyclic amine building blocks A-L.…”

“…[11,12] Another study outlined ah yperactivity of the serotoninergic system in frontotemporald ementia,a nN D similar to but distinct from AD, in which 5-HT receptors are preserved from neuronal tissue damage. [18] As we considered this composite and challenging scenario, we decided to investigate an ew series of compounds sharing ak nown synthetic tricyclics caffold that is easily accessible in our laboratories [19] as possibly selective antagonists of 5-HT 1A receptors, [20] keeping in mind the high chance that they would also have antagonist activity at the a 1A and D 2 receptors. [13] However,i th as to be admitted that the role and therapeutic potential of 5-HT 1A antagonists in AD have not been fully clarified yet and, despite the fact that many studies have supported their potential beneficial effects, clinicalt rial outcomes have been quite disappointing.…”

Synthesis and biological evaluation of some novel sulfamoylphenyl-pyridazinone as anti-inflammatory agents (Part-II)

“…They also act as cytotoxic (cell-killing) agents and antihormonal drugs, which reduce the proliferation of the tumors [15][16] . The sulfonamides constitute an important class of drugs, with several types of pharmacological agents possessing antibacterial 17 , anti-carbonic anhydrase 18,19 , diuretic 18,20 , hypoglycemic 21 , antithyroid 22 , and antiprotons activities [23][24][25] . A large number of structurally novel sulfonamide derivatives have recently been reported to show substantial antitumor activity, both in vitro and/ or in vivo.…”

Synthesis, Characterization and Antioxidant Activities of Novel 1-(Morpholine-4-Yl-Methyl)-3-Alkyl(aryl)-4-[4-(Dimethylamino)-Benzylidenamino]-4,5-Dihydro-1h-1,2,4-Triazol-5-Ones

“…anticancer (2,3), antibacterial (4,5), antimycobacterial (6), anti-HIV (7), antiinflammatory (8,9), analgesic (10,11), antifungal (12,13), antitumor (14,15), antiviral (16), antidepressant (17), antiulcer (18), anticonvulsant (19), antimalaria (20), and antioxidant activities (21).…”