6533b823fe1ef96bd127f64e
RESEARCH PRODUCT
Synthesis and cytotoxic activity of 3-[2-(1H-indol-3-yl)-1,3-thiazol-4-yl]-1H-pyrrolo[3,2-c]pyridine hydrobromides, analogues of the marine alkaloid nortopsentin
Daniela CarboneCamilla PecoraroDaniele AielloAnna Carbonesubject
ChemistryStereochemistry5-azaindole Antitumor activity Marine bis-indolyl alkaloids Nortopsentin analogues ThiazoleAlkaloidOrganic ChemistryNortopsentin analogues5-azaindoleSettore CHIM/08 - Chimica FarmaceuticaMarine bis-indolyl alkaloidschemistry.chemical_compoundMarine bis-indolyl alkaloids nortopsentin analogues antitumor activity 5-azaindole thiazolePyridineCytotoxic T cellThiazoleAntitumor activitydescription
A new series of thiazole nortopsentin analogues with a 5-azaindole moiety was conveniently synthesized in good to excellent yields by an Hantzsch reaction between thioamides and α-bromoacetyl compounds. The cytotoxic activity of the new derivatives was tested against different human tumor cell lines of the NCI full panel. All tested compounds were active against all of the investigated cell lines showing GI50 values from micro to submicromolar levels. Some of the new analogues exhibited good selectivities against different NCI sub-panels.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2021-11-10 | Arkivoc |