- NOVEL CYTOTOXIC AGENTS AND CONJUGATES THEREOF
-
Provided herein are novel maytansinoid compounds of general formula I. Also provided herein are conjugates comprising the compounds linked to a binding protein via a linker, and conjugating reagents comprising the compounds attached via a linker to at least one functional group capable of reacting with a binding protein. Also provided herein are pharmaceutical compositions comprising the compounds and conjugates, therapeutic methods and uses involving the compounds and conjugates, for example in cancer therapy, and novel synthetic processes.
- -
-
-
- CONJUGATES AND CONJUGATING REAGENTS COMPRISING A LINKER THAT INCLUDES AT LEAST TWO (-CH2-CH2-0-) UNITS IN A RING
-
A conjugate comprising a protein or peptide conjugated to a therapeutic, diagnostic or labelling agent via a linker, characterised in that the linker includes at least two ~(CH2-CH2- 0-)~ units within a ring, said ring being attached via a single tethering atom within the ring to the rest of the linker, or said ring being attached via two or more tethering atoms within the ring to the rest of the linker at a single point.
- -
-
-
- FORMATION OF COMPLEXES BETWEEN AZA DERIVATIVES OF CROWN ETHERS AND PRIMARY ALKYLAMMONIUM SALTS. PART 8. 12-CROWN-4, 15-CROWN5, 21-CROWN-7, AND 24-CROWN-8 DERIVATIVES
-
The monoaza-crown ethers (3), (4), and (5) and the diaza-crown ethers (6), (7), (10), and (11) form complexes with primary alkylammonium thiocyanates in organic solvents.The diaza-15-crown-5 system (11) forms well defined 1:1 complexes with the cis-, cis-stereochemistry shown in (16) but the diaza-24-crown-8-derivative (7) forms a 2:1 complex (G:H ratio) with benzylammonium thiocyanate having the cis,cis,trans,trans-stereochemistry (17a).The diaza-24-crown-6 derivative (10) forms weak 1:1 complexes which apparently adopt the double nesting conformation (18).
- Johnson, Martin R.,Jones, Nigel F.,Sutherland, Ian O.
-
p. 1637 - 1644
(2007/10/02)
-