Reengineered tricyclic anti-cancer agents was written by Kastrinsky, David B.;Sangodkar, Jaya;Zaware, Nilesh;McClinch, Kimberly;Farrington, Caroline C.;Giannini, Heather M.;Izadmehr, Sudeh;Dhawan, Neil S.;Narla, Goutham;Ohlmeyer, Michael. And the article was included in Bioorganic & Medicinal Chemistry in 2015.Electric Literature of C6H7ClN2O3S2 This article mentions the following:
The phenothiazine and dibenzazepine tricyclics are potent neurotropic drugs with a documented but underutilized anti-cancer side effect. Reengineering these agents (TFP, CPZ, CIP) by replacing the basic amine with a neutral polar functional group (e.g., RTC-1, RTC-2) abrogated their CNS effects as demonstrated by in vitro pharmacol. assays and in vivo behavioral models. Further optimization generated several phenothiazines and dibenzazepines with improved anti-cancer potency, exemplified by RTC-5. This new lead demonstrated efficacy against a xenograft model of an EGFR driven cancer without the neurotropic effects exhibited by the parent mols. Its effects were attributed to concomitant neg. regulation of PI3K-AKT and RAS-ERK signaling. In the experiment, the researchers used many compounds, for example, 2-Acetamido-4-methylthiazole-5-sulfonyl chloride (cas: 69812-29-9Electric Literature of C6H7ClN2O3S2).
2-Acetamido-4-methylthiazole-5-sulfonyl chloride (cas: 69812-29-9) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Electric Literature of C6H7ClN2O3S2
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica