- Design and synthesis of 1,4-substituted 1H-1,2,3-triazolo-quinazolin-4(3H)-ones by Huisgen 1,3-dipolar cycloaddition with PI3Kγ isoform selective activity
-
A strategy for construction of medicinally important 1,4-substituted 1H-1,2,3-triazolo-quinazolin-4(3H)-ones has been devised and presented here. The compounds have been synthesized using one-pot multicomponent strategy under microwave assisted conditions. Triazolyl-quinazolinone based D-ring modified analogs are designed based on IC87114 scaffold, which is first known isoform selective inhibitor of PI3Kδ. Herein, we identified two triazolyl-quinazolinone compounds (5a and 5l) based on same scaffold with PI3Kγ specific inhibitory potential, the selectivity towards this isoform is well supported by in silico results, wherein, these compounds show better interaction and affinity and inhibitory activity for PI3Kγ rather than PI3Kδ. This repositioning of scaffold from PI3Kδ to PI3Kγ isoform can be very useful from medicinal chemistry and drug discovery perspective to unravel molecular interactions of this new scaffold in different cellular pathways.
- Srinivas,Singh Pathania, Anup,Mahajan, Priya,Verma, Praveen K.,Chobe, Santosh S.,Malik, Fayaz A.,Nargotra, Amit,Vishwakarma, Ram A.,Sawant, Sanghapal D.
-
p. 1005 - 1010
(2018/03/01)
-
- One-pot multicomponent synthesis of medicinally important purine quinazolinone derivatives
-
Herein, a protocol that involves microwave-assisted, multicomponent one-pot synthetic strategy for the construction of the medicinally important purine quinazolinone scaffold is reported. A series of compounds are prepared by cyclization and condensation
- Sawant, Sanghapal D.,Srinivas, Mahesuni,Reddy, G. Lakshma,Rao, V. Venkateswar,Singh, Parvinder Pal,Vishwakarma, Ram A.
-
supporting information
p. 6195 - 6198,4
(2012/12/12)
-
- One-pot multicomponent synthesis of medicinally important purine quinazolinone derivatives
-
Herein, a protocol that involves microwave-assisted, multicomponent one-pot synthetic strategy for the construction of the medicinally important purine quinazolinone scaffold is reported. A series of compounds are prepared by cyclization and condensation
- Sawant, Sanghapal D.,Srinivas, Mahesuni,Reddy, G.Lakshma,Rao, V.Venkateswar,Singh, Parvinder Pal,Vishwakarma, Ram A.
-
supporting information
p. 6195 - 6198
(2013/01/14)
-
- INHIBITORS OF PI3K-DELTA AND METHODS OF THEIR USE AND MANUFACTURE
-
The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds
- -
-
-
- METHODS AND COMPOSITIONS FOR TREATMENT OF OPHTHALMIC CONDITIONS
-
The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating signal transduction by certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PB kinase in a
- -
-
-
- Inhibitors of human phosphatidylinositol 3-kinase delta
-
Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.
- -
-
Page column 65-66
(2008/06/13)
-