European Journal of Medicinal Chemistry p. 236 - 246 (2018)
Update date:2022-08-28
Topics:
Parrino, Barbara
Ullo, Salviana
Attanzio, Alessandro
Cascioferro, Stella
Spanò, Virginia
Carbone, Anna
Montalbano, Alessandra
Barraja, Paola
Cirrincione, Girolamo
Tesoriere, Luisa
Diana, Patrizia
Pyrrolizinones represent an interesting class of compounds with varied degrees of structural complexity and pharmacological activity. Among these, 9H-pyrido[2,3-b]pyrrolizin-9-one, tripentone analogs, recently reported by us, showed significant antiproliferative activity against human tumor cell lines, inducing apoptosis and not affecting viability of Caco-2 differentiated in normal intestinal-like cells. Considering their interesting biological activity, their 5H-pyrido[3,2-b]pyrrolizin-5-one analogs were efficiently synthesized in good to excellent yields (61–91%). All tripentone derivatives were tested to assess their cytotoxicity against two human tumor cell lines, HCT-116 (human colorectal carcinoma) and MCF-7 (human breast cancer). The most active derivatives, with IC50 ranging from 0.11 to 16.11 μM, did not affect viability of Caco-2 differentiated in normal intestinal-like cells, suggesting tumor cells as the main target of their cytotoxic action. The same compounds, further investigated, showed that they did not exert necrotic effects, while induced a clear shift of viable cells towards early apoptosis confining the cells in the mitotic phases.
View Morewebsite:http://www.sjzthld.com
Contact:86-311-66699812
Address:NO.600 ZHONGSHAN EAST ROAD SHIJIAZHUANG
Wuhan Hanye Chemical New Material Co.,Ltd
Contact:+86-27-85308141
Address:LiuDian, Panlongcheng Economic Development Zone, HuangPi district, Wuhan, Hubei 430311 P.R.China
Changsha Huajing Powdery Material Technological Co., Ltd.
Contact:86-731-88879686
Address:Building 2, West Garden, Main Campus of Central South University, Changsha, Hunan Province, China
Jiangsu Allyrise Pharmaceutical Co., Ltd.
Contact:+86-523-86818997
Address:Taizhou,Jiangsu Province,CHINA
website:http://www.chinabarton.com
Contact:+86-573-82719618
Address:No. 162 Fumin Road, Honghe Town,
Doi:10.1016/S0040-4020(99)80001-5
(1999)Doi:10.1039/J29690000517
(1969)Doi:10.3390/molecules18078358
(2013)Doi:10.1515/znb-2006-1204
(2006)Doi:10.1016/j.ica.2013.12.019
(2014)Doi:10.1016/j.ica.2006.11.010
(2007)