Antitumor benzothiazoles. 26. 2-(3,4-Dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines was written by Mortimer, Catriona G.;Wells, Geoffrey;Crochard, Jean-Philippe;Stone, Erica L.;Bradshaw, Tracey D.;Stevens, Malcolm F. G.;Westwell, Andrew D.. And the article was included in Journal of Medicinal Chemistry in 2006.Category: iodides-buliding-blocks This article mentions the following:
A series of new 2-phenylbenzothiazoles has been synthesized on the basis of the discovery of the potent and selective in vitro antitumor properties of 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (I; GW 610, NSC 721648). Synthesis of analogs substituted in the benzothiazole ring was achieved via the reaction of o-aminothiophenol disulfides with substituted benzaldehydes under reducing conditions. Compounds were evaluated in vitro in four human cancer cell lines, and I was found to possess exquisitely potent antiproliferative activity (GI50 < 0.1 nM for MCF-7 and MDA 468). Potent and selective activity was also observed in the NCI 60 human cancer cell line panel. Structure-activity relationships study established that I stands on a pinnacle of potent activity, with most structural variations having a deactivating in vitro effect. Mechanistically, this new series of agents contrasts with the previously reported 2-(4-aminophenyl)benzothiazoles; I is not reliant on induction of CYP1A1 expression for antitumor activity. In the experiment, the researchers used many compounds, for example, 3-Iodo-4-methoxybenzaldehyde (cas: 2314-37-6Category: iodides-buliding-blocks).
3-Iodo-4-methoxybenzaldehyde (cas: 2314-37-6) belongs to iodide derivatives. In general, organic iodides are light-sensitive and turn yellow during storage, owing to the formation of iodine. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.Category: iodides-buliding-blocks
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com