Nudelman, Abraham published the artcileProdrugs of butyric acid. Novel derivatives possessing increased aqueous solubility and potential for treating cancer and blood diseases, HPLC of Formula: 122110-53-6, the publication is European Journal of Medicinal Chemistry (2001), 36(1), 63-74, database is CAplus and MEDLINE.
The synthesis and biol. activities of acidic, basic and neutral types of butyric acid (BA) prodrugs possessing increased aqueous solubility are described. The compounds are butyroyloxyalkyl derivatives of carboxylic acids, which possess functionalities suitable for aqueous solubilization. The anticancer activity of the prodrugs in vitro was evaluated by examining their effect on the growth of human colon, breast and pancreatic carcinoma cell lines, and their solubility in aqueous media was determined The most promising compounds, with respect to activity and solubility, were the butyroyloxymethyl esters of glutaric and nicotinic acids and phosphoric acid as its di-Et ester, which displayed IC50 values of 100 μM or lower. These prodrugs are expected to release formaldehyde upon metabolic hydrolysis. The corresponding butyroyloxymethyl esters that release acetaldehyde upon metabolism were significantly less potent. A similar correlation was observed for growth inhibition of the human prostate carcinoma cell lines PC-3 and LnCap and for induction of differentiation and apoptosis in the human myeloid leukemia cell line HL-60. The higher biol. activity of the formaldehyde-releasing prodrugs I and II was further confirmed when induction of Hb synthesis in the human erythroleukemic cell line K562 was measured. Moreover, a therapeutic index (IC50/ED50) of 5 was observed The acute i.p. toxicity LD50 in mice for I, III, II and IV was similar and in the range of 400-600 mg kg-1. The results obtained support the potential use of the butyric acid prodrugs for the treatment of neoplastic diseases and β-globin disorders.
European Journal of Medicinal Chemistry published new progress about 122110-53-6. 122110-53-6 belongs to esters-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Ester,Inhibitor, name is (Pivaloyloxy)methyl butyrate, and the molecular formula is C10H18O4, HPLC of Formula: 122110-53-6.
Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics