Betulinic Acid Derivatives: A New Class of Specific Inhibitors of Human Immunodeficiency Virus Type 1 Entry
摘要:
A novel series of omega-aminoalkanoic acid derivatives of betulinic acid were synthesized and evaluated for their activity against human immunodeficiency virus (HIV). The anti-HIV-1 activity of several members of this new series was found to be in the nanomolar range in CEM 4 and MT-4 cell cultures. The optimization of the omega-aminoalkanoic acid side chain is described. The presence of an amide function within the side chain was found important for optimal activity. RPR 103611 (14g), a statine derivative, was found to be inactive against HIV-1 protease, reverse transcriptase, and integrase as well as on gp120/CD4 binding. ''Time of addition'' experiments suggested interaction with an early step of HIV-1 replication. As syncytium formation, but not virus-cell binding, seems to be affected, betulinic acid derivatives are assumed to interact with the postbinding virus-cell fusion process.
Next-Generation Diprovocims with Potent Human and Murine TLR1/TLR2 Agonist Activity That Activate the Innate and Adaptive Immune Response
作者:Ming-Hsiu Yang、Jamie L. Russell、Yuto Mifune、Ying Wang、Hexin Shi、Eva Marie Y. Moresco、Daniel J. Siegwart、Bruce Beutler、Dale L. Boger
DOI:10.1021/acs.jmedchem.2c00419
日期:2022.7.14
US5468888A
申请人:——
公开号:US5468888A
公开(公告)日:1995-11-21
[EN] TETRAHYDROISOQUINOLINE HETEROBIFUNCTIONAL BCL-XL DEGRADERS<br/>[FR] AGENTS DE DÉGRADATION DE BCL-XL HÉTÉROBIFONCTIONNELS À BASE DE TÉTRAHYDROISOQUINOLÉINE
申请人:[en]TREELINE BIOSCIENCES, INC.
公开号:WO2023215449A1
公开(公告)日:2023-11-09
This disclosure provides compounds of Formula (I) or pharmaceutically acceptable salts thereof, that induce degradation of a BCL-XLprotein. These are useful, for example, for treating a cancer in a subject (e.g., a human). This disclosure also provides compositions containing the compounds provided herein as well as methods of using and making the same.
Betulinic Acid Derivatives: A New Class of Specific Inhibitors of Human Immunodeficiency Virus Type 1 Entry
作者:Françoise Soler、Christèle Poujade、Michel Evers、Jean-Christophe Carry、Yvette Hénin、Anne Bousseau、Thierry Huet、Rudi Pauwels、Erik De Clercq、Jean-François Mayaux、Jean-Bernard Le Pecq、Norbert Dereu
DOI:10.1021/jm950669u
日期:1996.1.1
A novel series of omega-aminoalkanoic acid derivatives of betulinic acid were synthesized and evaluated for their activity against human immunodeficiency virus (HIV). The anti-HIV-1 activity of several members of this new series was found to be in the nanomolar range in CEM 4 and MT-4 cell cultures. The optimization of the omega-aminoalkanoic acid side chain is described. The presence of an amide function within the side chain was found important for optimal activity. RPR 103611 (14g), a statine derivative, was found to be inactive against HIV-1 protease, reverse transcriptase, and integrase as well as on gp120/CD4 binding. ''Time of addition'' experiments suggested interaction with an early step of HIV-1 replication. As syncytium formation, but not virus-cell binding, seems to be affected, betulinic acid derivatives are assumed to interact with the postbinding virus-cell fusion process.
Lupane derivatives, their preparation and the pharmaceutical
申请人:Rhone-Poulenc Rorer S.A.
公开号:US05468888A1
公开(公告)日:1995-11-21
The present invention relates to new lupane dervivatives of the general formula: ##STR1## to their salts, to their preparation and to the pharmaceutical compositions which contain them.