140693-22-7Relevant academic research and scientific papers
CROSS-LINKED PYRROLOBENZODIAZEPINE DIMER (PBD) DERIVATIVE AND ITS CONJUGATES
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Page/Page column 169, (2020/01/31)
A novel cross-linked cytotoxic agents, pyrrolobenzo-diazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.
CONJUGATION LINKERS CONTAINING 2,3-DIAMINOSUCCINYL GROUP
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Page/Page column 315, (2020/05/19)
Provided is a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (adual-linker) containing a 2, 3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.
NOVEL CYTOTOXIC AGENTS FOR CONJUGATION OF DRUGS TO CELL BINDING MOLECULE
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Page/Page column 91, (2015/03/16)
Provided are cytotoxic agents, pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives, their conjugates with a cell-binding agent, the preparation and the therapeutic uses in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.
Synthesis, DNA-binding ability and anticancer activity of benzothiazole/benzoxazole-pyrrolo[2,1-c][1,4]benzodiazepine conjugates
Kamal, Ahmed,Reddy, K. Srinivasa,Khan, M. Naseer A.,Shetti, Rajesh V.C.R.N.C.,Ramaiah, M. Janaki,Pushpavalli,Srinivas, Chatla,Pal-Bhadra, Manika,Chourasia, Mukesh,Sastry, G. Narahari,Juvekar, Aarti,Zingde, Surekha,Barkume, Madan
scheme or table, p. 4747 - 4761 (2010/08/20)
A series of benzothiazole and benzoxazole linked pyrrolobenzodiazepine conjugates attached through different alkane or alkylamide spacers was prepared. Their anticancer activity, DNA thermal denaturation studies, restriction endonuclease digestion assay and flow cytometric analysis in human melanoma cell line (A375) were investigated. One of the compounds of the series 17d showed significant anticancer activity with promising DNA-binding ability and apoptosis caused G0/G1 phase arrest at sub-micromolar concentrations. To ascertain the binding mode and understand the structural requirement of DNA binding interaction, molecular docking studies using gold program and more rigorous 2 ns molecular dynamic simulations using Molecular Mechanics-Poisson-Boltzman Surface Area (MM-PBSA) approach including the explicit solvent were carried out. Further, the compound 17d was evaluated for in vivo efficacy studies in human colon cancer HT29 xenograft mice.
Synthesis of C8-C8/C2-C8-linked triazolo pyrrolobenzodiazepine dimers by employing 'click' chemistry and their DNA-binding affinity
Kamal, Ahmed,Prabhakar,Shankaraiah,Reddy, Ch. Ratna,Reddy, P. Venkat
, p. 3620 - 3624 (2008/09/21)
A series of 1,2,3-triazole-containing pyrrolo[2,1-c][1,4]benzodiazepine dimers have been prepared efficiently by employing a 'click' chemistry protocol. This method involves 1,3-dipolar cycloaddition of terminal alkynes with organic azides using a Cu(I)-c
Design, synthesis, and evaluation of mixed imine-amine pyrrolobenzodiazepine dimers with efficient DNA binding affinity and potent cytotoxicity
Kamal, Ahmed,Ramesh,Srinivas,Ramulu,Laxman,Rehana, Tasneem,Deepak,Achary,Nagarajaram
, p. 5427 - 5436 (2007/10/03)
Synthesis of mixed imine-amine pyrrolobenzodiazepine (PBD) dimers that are comprised of DC-81 and secondary amine (N10) of DC-81 subunits tethered to their C8 positions through alkanedioxy linkers (comprised of three and five carbons) is described. These
Design and synthesis of C-8 linked pyrrolobenzodiazepine-naphthalimide hybrids as anti-tumour agents
Kamal, Ahmed,Reddy,Reddy, G.Suresh Kumar,Ramesh
, p. 1933 - 1935 (2007/10/03)
The facile synthesis of C-8 linked pyrrolobenzodiazepine-naphthalimide hybrid analogues is described. The compounds are prepared with varying degrees of linker length in order to probe the structural requirements for optimal in vitro anti-tumour activity. Some of these new hybrid compounds showed higher cytotoxic activity than the existing natural and synthetic pyrrolo[2,1-c][1,4]benzodiazepines.
An efficient synthesis of pyrrolo[2,1-c][1,4]benzodiazepine antibiotics via reductive cyclization
Kamal, Ahmed,Reddy, B. S. Nararyan,Reddy, B. S. Praveen
, p. 1825 - 1828 (2007/10/03)
A new and convenient one-pot synthesis of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) ring system has been achieved by a reductive cyclization employing N,N-dimethylhydrazine and FeCl3.6H2O in good yields.
Novel biocatalytic reduction of aryl azides: Chemoenzymatic synthesis of pyrrolo[2,1-c][1,4]benzodiazepine antibiotics
Kamal, Ahmed,Damayanthi,Reddy, B. S. Narayan,Lakminarayana,Reddy, B. S. Praveen
, p. 1015 - 1016 (2007/10/03)
The chemoselective reduction of aryl azides to aryl amines, and the synthesis of the imine-containing pyrrolo[2,1-c][1-4]benzodiazepine DNA-binding antitumour antibiotics by selective biocatalytic reductive cyclization of azido aldehydes, has been achieved by employing baker's yeast.
A new facile procedure for the preparation of pyrrolo[2,1-c][1,4]benzodiazepines : Synthesis of the antibiotic DC-81 and its thio analogue
Kamal, Ahmed,Reddy, B. S. Praveen,Reddy, B. S. Narayan
, p. 2281 - 2284 (2007/10/03)
An efficient synthesis of the imine form of the pyrrolo[2,1-c][1,4] benzodiazepine ring system based on a new reductive cyclization procedure is described. The naturally occuring antibiotic DC-81(5c) and its 5-thio analogue (7c) have also been synthesized to illustrate the usefulness of this methodology.
