Synthesis, characterization and biological evaluation of bile acid-aromatic/heteroaromatic amides linked via amino acids as anti-cancer agents

Add time:08/02/2019    Source:sciencedirect.com

A series of bile acid (Cholic acid and Deoxycholic acid) aryl/heteroaryl amides linked via α-amino acid were synthesized and tested against 3 human cancer cell-lines (HT29, MDAMB231, U87MG) and 1 human normal cell line (HEK293T). Some of the conjugates showed promising results to be new anticancer agents with good in vitro results. More specifically, Cholic acid derivatives 6a (1.35 μM), 6c (1.41 μM) and 6m (4.52 μM) possessing phenyl, benzothiazole and 4-methylphenyl groups showed fairly good activity against the breast cancer cell line with respect to Cisplatin (7.21 μM) and comparable with respect to Doxorubicin (1 μM), while 6e (2.49 μM), 6i (2.46 μM) and 6m (1.62 μM) showed better activity against glioblastoma cancer cell line with respect to both Cisplatin (2.60 μM) and Doxorubicin (3.78 μM) drugs used as standards. Greater than 65% of the compounds were found to be safer on human normal cell line.

We also recommend Trading Suppliers and Manufacturers of methyl amino(4-methylphenyl)acetate hydrochloride (cas 134722-09-1). Pls Click Website Link as below: cas 134722-09-1 suppliers

Prev:Branching cascades provide access to two amino-oxazoline compound libraries
Next:Agonist and antagonist activities of the leukotriene analogue BAY U9773 (cas 134733-55-4) in guinea pig lung parenchyma)