|
Type |
Poster Presentation |
Area |
Medicinal Chemistry |
Room No. |
Event Hall |
Time |
4월 19일 (목요일) 11:00~12:30 |
Code |
MEDI.P-640 |
Subject |
Synthesis and Molecular Modeling Studies of N`-Hydroxyindazolecarboximidamides as Novel
Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors |
Authors |
AhRa Go, HEE NANG CHOI, Jong Yeon Hwang*, Hyunjin Kim1, jae du ha2 Center for Medicinal Chemistry, Korea Research Institute of Chemical Technology, Korea 1Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Korea 2WCI, Korea Research Institute of Chemical Technology, Korea |
Abstract |
Indoleamine 2,3-dioxygenase 1 (IDO1) is an immunosuppressive enzyme that is highly
overexpressed in various cancer cells and antigen-presenting cells. It has emerged as an attractive
therapeutic target for cancer immunotherapy, which has prompted high interest in the development
of small-molecule inhibitors. To discover novel IDO1 inhibitors, we designed and synthesized a
series of N0-hydroxyindazolecarboximidamides. Among the compounds synthesized, compound
8a inhibited both tryptophan depletion and kynurenine production through the IDO1 enzyme.
Molecular docking studies revealed that 8a binds to IDO1 with the same binding mode as the
analog, epacadostat (INCB24360). Here, we report the synthesis and biological evaluation of these
hydroxyindazolecarboximidamides and present the molecular docking study of 8a with IDO1. |
E-mail |
rhrkfk@hanmail.net |
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