[EN] ASYMMETRIC BISAMINOQUINOLINES AND BISAMINOQUINOLINES WITH VARIED LINKERS AS AUTOPHAGY INHIBITORS FOR CANCER AND OTHER THERAPY [FR] BISAMINOQUINOLINES ASYMÉTRIQUES ET BISAMINOQUINOLINES COMPORTANT DIVERSES SÉQUENCES DE LIAISON POUVANT ÊTRE UTILISÉES EN TANT QU'INHIBITEURS DE L'AUTOPHAGIE POUR LE TRAITEMENT DU CANCER ET D'AUTRES MALADIES
[EN] ASYMMETRIC BISAMINOQUINOLINES AND BISAMINOQUINOLINES WITH VARIED LINKERS AS AUTOPHAGY INHIBITORS FOR CANCER AND OTHER THERAPY [FR] BISAMINOQUINOLINES ASYMÉTRIQUES ET BISAMINOQUINOLINES COMPORTANT DIVERSES SÉQUENCES DE LIAISON POUVANT ÊTRE UTILISÉES EN TANT QU'INHIBITEURS DE L'AUTOPHAGIE POUR LE TRAITEMENT DU CANCER ET D'AUTRES MALADIES
Asymmetric bisaminoquinolines and bisaminoquinolines with varied linkers as autophagy inhibitors for cancer and other therapy
申请人:THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
公开号:US10221140B2
公开(公告)日:2019-03-05
The invention provides novel asymmetric and symmetric bisaminoquinolmes and related compounds, methods of treatment and syntheses. The novel compounds exhibit effective anticancer activity and are useful in the treatment of a variety of autophagy-related disorders.
Dimeric quinacrine derivatives as autophagy inhibitors for cancer therapy
申请人:THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
公开号:US10774047B2
公开(公告)日:2020-09-15
The invention provides dimeric quinacrine derivatives and related compounds and compositions, methods of treatment and syntheses. The novel compounds exhibit unexpected anticancer activity and are useful in the treatment of a variety of autophagy-related disorders.
Bisquinoline heteroalkanediamines were structurally modified in order to study the effects of enhanced bulkiness and rigidity on both their activity on strains of Plasmodium falciparum expressing different degrees of chloroquine (CQ) resistance and their cytotoxicity toward mammalian cells. While cyclization yielded molecules of greater rigidity that were not more active than their linear counterparts, they were characterized by an absence of cytotoxicity. Alternatively, dimerization of these compounds led to tetraquinolines that are very potent for CQ-resistant strains and noncytotoxic.
ASYMMETRIC BISAMINOQUINOLINES AND BISAMINOQUINOLINES WITH VARIED LINKERS AS AUTOPHAGY INHIBITORS FOR CANCER AND OTHER THERAPY
申请人:The Trustees of The University of Pennsylvania
公开号:EP3177595B1
公开(公告)日:2021-02-24
DIMERIC QUINACRINE DERIVATIVES AS AUTOPHAGY INHIBITORS FOR CANCER THERAPY
申请人:The Trustees of The University of Pennsylvania