30018-16-7Relevant articles and documents
A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
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Paragraph 000275; 000276, (2021/03/02)
The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
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Page/Page column 10; 164, (2019/07/17)
The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
Close the ring to break the cycle: Tandem quinolone-alkyne-cyclisation gives access to tricyclic pyrrolo[1,2-: A] quinolin-5-ones with potent anti-protozoal activity
Szamosvári, Dávid,Sylvester, Kayla,Schmid, Philipp,Lu, Kuan-Yi,Derbyshire, Emily R.,B?ttcher, Thomas
supporting information, p. 7009 - 7012 (2019/06/20)
Expanding the chemical space of quinolones led to a tandem quinolone-alkyne-cyclisation reaction allowing chemoselective control of the synthesis of tricyclic pyrrolo[1,2-a]quinolin-5-ones. Importantly, we discovered anti-protozoal activity against Plasmodium and Toxoplasma with specific potency of one of the compounds against the liver stage of the malaria parasite in the nanomolar range.