A new series of adamantanyl-1,3-thiazole and 1,3,4-oxadiazole derivatives (6a-l), bearing various aryl groups has been synthesized from adamantan-1-nitrile in four steps. All the compounds were evaluated, in vitro, for antiproliferative activity against a large panel of human tumor-derived cell lines. Compounds 6e exhibited activity against human splenic B-lymphoblastoid (WIL-2NS) and human acute B-lymphoblastic leukemia (CCRF-SB) cell lines with CC50 = 68 and 42 μM, respectively. Compound 61 showed activity against CCRF-SB cell lines with CC50 = 51 μM. All the other compounds were found inactive.
Synthesis and in vitro antiproliferative activity of new adamantylthiazolyl-1,3,4-oxadiazoles
LODDO, ROBERTA;
2009-01-01
Abstract
A new series of adamantanyl-1,3-thiazole and 1,3,4-oxadiazole derivatives (6a-l), bearing various aryl groups has been synthesized from adamantan-1-nitrile in four steps. All the compounds were evaluated, in vitro, for antiproliferative activity against a large panel of human tumor-derived cell lines. Compounds 6e exhibited activity against human splenic B-lymphoblastoid (WIL-2NS) and human acute B-lymphoblastic leukemia (CCRF-SB) cell lines with CC50 = 68 and 42 μM, respectively. Compound 61 showed activity against CCRF-SB cell lines with CC50 = 51 μM. All the other compounds were found inactive.
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