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 MoreSuqian Ruixing Chemical Co., Ltd.
Contact:+86-527-80805666(总机);84836008(销售)
Address:3 Jingsilu, Zone north, Hubin Xincheng Development Park, Suqian, China
Suzhou Howsine Biological Technology Co.,Ltd(expird)
website:http://www.howsine.com
Contact:86-512-67262751
Address:No 3,Weihua Road ,Suzhou Industrial Park ,Jiangsu ,China.
Nanjing Capatue Chemical Co., Ltd
Contact:+86-25-86371192 +86-025-85720158
Address:No.20 Jiangjun Avenue, Jiangning Economic & Technical Development Zone
Quhua Zhongxing Refrigeration Technology Co.,Ltd.
Contact:+86-5708886618
Address:318 Bulding 2, No.866 Quhua Rd.,Kecheng District
Nanjing Zelang Medical Technology Co. Ltd
Contact:86-25-83063290/13770714480
Address:Ganjiabian 108# 01 Unit,701-702 room,Yao Hua Street,Qixia District,Nanjing,Jiangsu,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)