Bioorganic Chemistry p. 1 - 14 (2019)
Update date:2022-08-16
Topics:
Ali, Ghada M.E.
Ibrahim, Diaa A.
Elmetwali, Amira M.
Ismail, Nasser S.M.
Different series of novel pyrazole and pyrazolo[1,5-a] pyrimidine derivatives (2a-g), (3a-c), (7a-d) and (10a-e) were designed, synthesized and evaluated for their ability to inhibit CDK2/cyclin A2 enzyme in vitro. In addition, the cytotoxicity of the newly synthesized compounds was screened against four different human cancer cell lines. The CDK2/cyclin A2 enzyme inhibitory activity revealed that compounds (2d) and (2 g) are among the most active with inhibitory activity values of 60% and 40%, respectively, while compounds (7d) and (10b) exhibited the highest activity among the newly synthesized derivatives against four tumor cell lines (HepG2, MCF-7, A549 and Caco2) with IC50 values 24.24, 14.12, 30.03 and 29.27 μM and 17.12, 10.05, 29.95 and 25.24 μM, respectively. Flow cytometry cell cycle assay was carried for compounds (7d) and (10b) to investigate their apoptotic activity. The obtained results revealed that they induced cell-cycle arrest in the G0-G1phase and reinforced apoptotic DNA fragmentation. Molecular modeling studies have been carried out to gain further understanding the binding mode of the target compounds together with field alignment to define the similar field properties.
View MoreContact:+86--29-82745382
Address:Development Area Of Lantian Country,Xi'an Shanxi.China
Anhui Dexinjia Biopharm Co., Ltd
Contact:+86-531-82375818
Address:9 Hexie Road, kaifaqu, Taihe
Henan zhongda Biological Engineering Co., Ltd
Contact:86-28-18109029985
Address:shenzhou road,xuedian industrial estate,zhengzhou city,henan province CHN
Shijiazhuang Frontierchem Co., Ltd.
Contact:+86-311-89271196
Address:4-4-202 No.15 Biandian Street,Shijiazhuang
Tangshan Moneide Trading Co., Ltd.
Contact:+86-315-8309571
Address:2-7-420 Jidong Building Materials Commercial Center, Tangshan, Hebei, 064000 China
Doi:10.1039/CT8793500012
(1879)Doi:10.1021/op500327t
(2015)Doi:10.1039/c9cc06822h
(2019)Doi:10.1021/acs.inorgchem.7b01763
(2017)Doi:10.1039/c7nj03240d
(2018)Doi:10.1007/BF01151265
()