European Journal of Medicinal Chemistry p. 201 - 208 (2014)
Update date:2022-08-15
Topics:
Reddy, G. Lakshma
Guru, Santosh Kumar
Srinivas
Pathania, Anup Singh
Mahajan, Priya
Nargotra, Amit
Bhushan, Shashi
Vishwakarma, Ram A.
Sawant, Sanghapal D.
A microwave assisted strategy for synthesis of series of 1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones has been developed and their biological evaluation as anticancer agents is described. The synthetic protocol involves simple procedure by oxidative coupling of 4-amino-1-methyl-3-propyl-1H-pyrazole- 5-carboxamide with different aldehydes in presence of K2S 2O8 offering 5-substituted-1H-pyrazolo[4,3-d]pyrimidin- 7(6H)-one compounds in excellent yields. The in vitro anticancer activity screening against human cancer cell lines HeLa, CAKI-I, PC-3, MiaPaca-2, A549 gave good results. The in detailed mechanistic correlation studies of compound 3m revealed that the compound shows anticancer activity through apoptosis mechanism and also inhibits mTOR with nonomolar potency. The design was based on docking with mTOR protein. The concentration dependent cell cycle analysis, western blotting experiment and nuclear cell morphology studies have been described.
View MoreContact:+86-25-85281586
Address:13F,Bld2#,South of Longpan Road
Changzhou Anyi Biochem Co., Ltd.
Contact:+86-519-88836158
Address:no,51 caoda
Changzhou Kingyo Chemical Corporation Ltd.
website:http://www.kingyochem.com
Contact:+86-519-85105717
Address:19# Wuqing North Road, Changzhou , Jiangsu, China
Taizhou Elitechemie MediPharma Technology Co.,Ltd.
Contact:+86-523-86810021
Address:Building G14,NO.1 Avenue,China Medical City, Taizhou, Jiangsu,China
Contact:+86-310-7092106
Address:Quzhou Modern & New Industrial Park, Handan, Hebei 057250, China
Doi:10.1002/ardp.19943271202
(1994)Doi:10.1016/j.ejmech.2014.04.030
(2014)Doi:10.1021/jo01191a004
(1943)Doi:10.1021/jo026649z
(2003)Doi:10.1002/adsc.201300925
(2014)Doi:10.1021/jo500771g
(2014)