Raffa Demetrio, Maggio Benedetta, Plescia Fabiana, Cascioferro Stella, Raimondi Maria Valeria, Cancemi Gabriella, D'Anneo Antonella, Lauricella Marianna, Cusimano Maria Grazia, Bai Ruoli, Hamel Ernest, Daidone Giuseppe
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123 Palermo, Italy.
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123 Palermo, Italy.
Bioorg Med Chem. 2015 Oct 1;23(19):6305-16. doi: 10.1016/j.bmc.2015.08.027. Epub 2015 Aug 28.
Several new 2-(2-phenoxyacetamido)benzamides 17a-v, 21 and 22 were synthesized by stirring in pyridine the acid chlorides 16a-e and the appropriate5-R-4-R₁-2-aminobenzamide 15a-e and initially evaluated in vitro for antiproliferative activity against the K562 (human chronic myelogenous leukemia) cell line. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). The most active compounds caused an arrest of K562 cells in the G0-G1 phase of cell cycle and induction of apoptosis, which was mediated by caspase activation.
通过在吡啶中搅拌酰氯16a - e与相应的5 - R - 4 - R₁ - 2 -氨基苯甲酰胺15a - e,合成了几种新的2 - (2 -苯氧基乙酰氨基)苯甲酰胺17a - v、21和22,并初步在体外评估了它们对K562(人慢性髓性白血病)细胞系的抗增殖活性。对一些合成化合物进行了体外抗增殖活性评估,其针对源自九种临床分离癌症类型(白血病、非小细胞肺癌、结肠癌、中枢神经系统癌、黑色素瘤、卵巢癌、肾癌、前列腺癌和乳腺癌)的完整NCI肿瘤细胞系面板。活性最强的化合物导致K562细胞在细胞周期的G0 - G1期停滞并诱导凋亡,这是由半胱天冬酶激活介导的。