摘要 |
<p>Cancer is one of the major causes of death worldwide. Although many advances have been made in the treatment and management of the disease, the existence of chemotherapy-resistance means there is still a great need to develop new strategies and drugs for its treatment. Provided herein are synthetic derivatives of combretastatin A-4, in particular those in which the aromatic rings are locked into a non-isomerisable active conformation, thus resulting in improved, stable compounds. The novel compounds are structurally related to combretastatin A-4 (CA-4) and lock the rings into the known active conformation by means of a four membered nitrogen containing heterocyclic ring, such as a beta-lactam ring, incorporated into the standard CA-4 structure. The compounds exhibit potent anti-cancer activity.</p> |
申请人 |
THE PROVOST, FELLOWS AND SCHOLARS OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH, NEAR DUBLIN;MEEGAN, MARY J.;ZISTERER, DANIELA;CARR, MIRIAM;GREENE, THOMAS;O'BOYLE, NIAMH;GREENE, LISA |
发明人 |
MEEGAN, MARY J.;ZISTERER, DANIELA;CARR, MIRIAM;GREENE, THOMAS;O'BOYLE, NIAMH;GREENE, LISA |