Steroids p. 91 - 98 (2019)
Update date:2022-08-11
Topics:
Bildziukevich, Uladzimir
Rárová, Lucie
Janovská, Lucie
?aman, David
Wimmer, Zdeněk
Amides of betulinic acid with cystamine were synthesized to investigate their antimicrobial and antitumor activity, and their influence on the cell cycle and cell apoptosis. The former target amide (6) displayed cytotoxicity in CEM cell line after 72 h of treatment (IC50 = 3.0 ± 0.7 μM; TI = 20), and induced apoptosis by caspase-3/7 activation in CEM cells. The latter target amide (9) displayed antimicrobial activity against Streptococcus mutans (MIC 3.125 μM; MBC 3.125 μM) and Bacillus cereus (MIC 25 μM; MBC 25 μM). The achieved results demonstrate enhancing of their biological activity over that of the parent compounds. However, two intermediate compounds (2 and 7) displayed either considerable cytotoxicity (2; 7.5 ± 0.8 μM; TI = 10, against G361) or antimicrobial activity (7; both against Actinomyces odontolycus and Clostridium perfrigens with MIC 12.5 μM and MBC 12.5 μM). The experimental data were compared with the in silico calculated physico-chemical and ADME parameters of the target compounds, including successful intermediates.
View MoreShanghai better-in Medical Technology Co.,LTD.
Contact:+86-21-38921049
Address:Lane 720 zhangjianggaoke cailun road, Pudong, Shanghai, room 513
website:http://www.oceanchem-group.com
Contact:86-536-8596048
Address:9th floor,Building B future Plaza, No.88.Fenghuang Street,Weifang,Shandong,China
Jingzhou TianHe Sci&Tech Chemical Co., Ltd.
Contact:86-716-8331612
Address:Jiangjin Road, #18, High-grade technology industries development district, Jingzhou city, Hubei province
Contact:+86-570-4336358
Address:No.87 Building,Tianqian,Sidu Town
Contact:86 513 85512619
Address:Rm.1306, Building A, Wenfeng Mansion,168 Gongnong Road, Nantong Jiangsu China
Doi:10.1039/c6ra21164j
(2016)Doi:10.1016/0040-4039(95)00229-6
(1995)Doi:10.1016/j.ica.2019.119208
(2020)Doi:10.1016/j.molcatb.2013.04.013
(2013)Doi:10.1021/jo00378a020
(1987)Doi:10.1128/aac.42.9.2245
(1998)