135609-17-5Relevant articles and documents
Synthesis of Highly Potent N-10 Amino-Linked DNA-Alkylating Indolinobenzodiazepine Antibody-Drug Conjugates (ADCs)
Archer, Katie E.,Reid, Emily E.,Shizuka, Manami,Woods, James,Harris, Luke,Maloney, Erin K.,Bartle, Laura M.,Ab, Olga,Wilhelm, Alan,Setiady, Yulius,Ponte, Jose F.,Singh, Rajeeva,Keating, Thomas A.,Chari, Ravi V. J.,Miller, Michael L.
, p. 1211 - 1215 (2019)
Indolinobenzodiazepine DNA alkylators (IGNs) are the cytotoxic payloads in antibody-drug conjugates (ADCs) currently undergoing Phase I clinical evaluation (IMGN779, IMGN632, and TAK164). These ADCs possess linkers that have been incorporated into a central substituted phenyl spacer. Here, we present an alternative strategy for the IGNs, linking through a carbamate at the readily available N-10 amine present in the monoimine containing dimer. As a result, we have designed a series of N-10 linked IGN ADCs with a wide range of in vitro potency and tolerability, which may allow us to better match an IGN with a particular target based on the potential dosing needs.
An alternative synthesis of benziporphyrins starting from isophthaloyl chloride
Darrow, William T.,Lash, Timothy D.
, p. 532 - 538 (2017)
An alternative route to benziporphyrins has been developed. Reaction of an α-unsubstituted pyrrole ethyl ester with isophthaloyl chloride in the presence of aluminum chloride afforded a diketone that underwent selective reduction with diborane to give a b
CYTOTOXIC BIS-BENZODIAZEPINE DERIVATIVES AND CONJUGATES THEREOF WITH CELL-BINDING AGENTS FOR INHIBITING ABNORMAL CELL GROWTH OR FOR TREATING PROLIFERATIVE DISEASES
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Paragraph 00343, (2020/10/20)
The invention relates to benzodiazepine derivatives with antiproliferative activity and more specifically to benzodiazepine compounds of formulae (I), (II), (TI) and (T2). The invention also provides conjugates of the benzodiazepine compounds linked to a
NOVEL BENZODIAZEPINE DERIVATIVES
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Page/Page column 114-116, (2010/08/18)
The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
