Feng Ni

US Patent:

20200048204, Feb 13, 2020

Filed:

Oct 4, 2017

Appl. No.:

16/339621

Inventors:

- Los Angeles CA, US
Feng NI - Los Angeles CA, US
Arunika Ishani EKANAYAKE - Inglewood CA, US

Assignee:

University of Southern California - Los Angeles CA

International Classification:

C07D 215/44
C07D 487/04
C07D 221/10

Abstract:

Despite its power in identifying highly potent ligands for select protein targets, conventional medicinal chemistry is limited by its low throughput and lack of proteomic selectivity information. We seek to develop a chemoproteomic approach for discovering covalent ligands for protein targets in an unbiased, high-throughput manner. Tripartite probe compounds composed of a heterocyclic core, an electrophilic ‘warhead’ and an alkyne tag have been designed and synthesized for covalently labeling and identifying targets in cells. We have developed a novel condensation reaction to prepare 2-chloromethylquinoline (2-CMQ), a novel electrophilic heterocycle. These chloromethylquinolines potently and covalently bind to a number of cellular protein targets including Prostaglandin E Synthase 2 (PTGES2), a critical regulator of cell proliferation, apoptosis, angiogenesis, inflammation, and immune surveillance.

US Patent:

20180064829, Mar 8, 2018

Filed:

Apr 2, 2016

Appl. No.:

15/563318

Inventors:

- Los Angeles CA, US
Boris A. Kashemirov - Los Angeles CA, US
Shuting Sun - Los Angeles CA, US
Feng Ni - Los Angeles CA, US

Assignee:

University of Southern California - Los Angeles CA

International Classification:

A61K 49/00
C07F 9/58
C07F 9/6506
C07F 9/6558
C07F 9/6561

Abstract:

Fluorescent probes based on N-heterocyclic bisphosphonates or their phosphonocarboxylate analogues are provided. The probes have variable spectroscopic properties, bone mineral binding affinities, and pharmacological activities. Methods for preparing the probes include the use of two complementary linking strategies, one involving an amino group and the other involving a chloride group as a precursor to an amino group. In other versions, bifunctional N-heterocyclic bisphosphonates are provided having an amino group and an azido group as linking moieties. In some versions, the linking chemistry allows attachment of a wide selection of fluorescent dyes in the visible to near-infrared range to any of three clinically important heterocyclic bisphosphonates.