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2 edition of Synthetic studies towards a novel DNA targeted cross-linking agent based on DC-81 and CC-1065 found in the catalog.

Synthetic studies towards a novel DNA targeted cross-linking agent based on DC-81 and CC-1065

Stephen John Croker

Synthetic studies towards a novel DNA targeted cross-linking agent based on DC-81 and CC-1065

by Stephen John Croker

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Published by University of Portsmouth, School of Pharmacy and Biomedical Sciences in Portsmouth .
Written in English


Edition Notes

Thesis (Ph.D.) - University of Portsmouth, 1997.

StatementStephen John Croker.
ID Numbers
Open LibraryOL16826113M

  A compound of the formula II: wherein: R′ 2 is CHR″ 2, where R″ 2 is H. R 6 and R 9 are H and R 7 is OMe; and the compound is a dimer with each monomer being the same and being of formula II, where the R 8 groups of the monomers form together a bridge having the formula —O—(CH 2) p —O—, where p is 5, linking the monomers. Cross-Linking in the Blood Clotting Process The first example is taken from the multistep process of blood clotting [ , , ]. In this case, in the final, thirteenth step (Figure 18) of the entire complex process, the two final protein intermediates 49 and 50 are linked to each other via a new side-chain amide bond [ ].

  In summary, several thiolactone-based synthetic approaches for the preparation and modification of a variety of functionalized polymers have been established. Download: Download full-size image; Fig. Overview of thiolactone-based synthetic approaches for the preparation and modification of various functionalized polymers. Antibodies and antibody-derived macromolecules have established themselves as the mainstay in protein-based therapeutic molecules (biologics). Our knowledge of the structure–function relationships of antibodies provides a platform for protein engineering that has been exploited to generate a wide range of biologics for a host of therapeutic indications.

Antineoplastic Agents: Substances that inhibit or prevent the proliferation of NEOPLASMS. Alkylating Agents: Highly reactive chemicals that introduce alkyl radicals into biologically active molecules and thereby prevent their proper are used as antineoplastic agents, but most are very toxic, with carcinogenic, mutagenic, teratogenic, and immunosuppressant actions. This banner text can have markup.. web; books; video; audio; software; images; Toggle navigation.


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Synthetic studies towards a novel DNA targeted cross-linking agent based on DC-81 and CC-1065 by Stephen John Croker Download PDF EPUB FB2

Synthetic studies towards a novel DNA targeted cross-linking agent based on DC and CC Thesis (Thesis) Find all citations by this author (default).Author: Croker Sj. Synthetic studies towards a novel DNA targeted cross-linking agent based on DC and CC By S.J.

Croker. Abstract. SIGLEAvailable from British Library Document Supply Centre-DSC:DXN / BLDSC - British Library Document Supply CentreGBUnited KingdoAuthor: S.J. Croker. Synthetic studies towards a novel DNA targeted cross-linking agent based on DC and CC Author: Croker, Stephen John. ISNI: Awarding Body: University of Portsmouth Current Institution: University of Portsmouth Date of Award.

Porphyrin-DNA cross-linking agent hybrids: Chemical synthesis and biological studies Article in Bioorganic & Medicinal Chemistry Letters 14(12). This symmetric molecule is a highly efficient minor groove interstrand DNA cross-linking agent (XL(50) = microM) that is fold more potent than melphalan.

SJG (NSC ), a novel rationally designed DNA minor groove interstrand cross-linking agent with potent and broad spectrum antitumor activity. Part 1: Cellular pharmacology, in vitro and. Design, Synthesis and in vitro Cytotoxicity Studies of Novel Pyrrolo[2,1][1,4]benzodiazepine-glycosylated Pyrrole and Imidazole Polyamide Conjugates.

This review presents the latest findings in the pursuit of novel synthetic DNA binders. This article provides recent coverage of major strategies (such as groove recognition, intercalation and cross-linking) adopted in the duplex DNA recognition by small molecules, with an emphasis on major works of the past few years.

The synthesis of the alkylating subunit of the DNA cross-linking agent, isochrysohermidin (2), and its subsequent incorporation into conjugates with distamycin A (1) are described.

The distance between the uramustine and distamycin frame is crucial for the cytotoxicity, in fact as the size of the linker spacer increases from n = 4–6, the cytotoxic activity is also enhanced, with IC 50 values in the range – μM. Compound 18f, with the longest linker length in the series, was the most active compound with an IC 50 value lower than that for distamycin.

Besides the abovementioned payloads, other molecules, which can be used as a DNA‐damaging agent in ADC synthesis, include SGD‐ (a cytotoxic DNA minor groove cross‐linking derivative of PBD dimers which is not an MDR1 substrate) (Kim & Kim, ), centanamycin (an indolecarboxamide synthesized as a less toxic analog of CC‐ and.

This molecule, which was designed to more closely follow the curvature of the minor groove, had a very high stabilizing effect on calf thymus DNA (i.e., ΔT m > °C), significant interstrand cross‐linking activity toward linear pBR plasmid DNA (i.e., >90 % cross‐linking for μ m drug concentration at DSB‐/DNA), and sub.

The novel C8-linked PBD–adenosine (PBD–ADN) hybrid (16) was prepared using a convergent synthetic approach and screened for antimicrobial, antiproliferative and DNA-binding activities.

The adenosine (11) and the PBD DC (5) units were synthesized separately and then linked via a pentynyl spacer at a later stage to give the title compound DNA-targeting indolinobenzodiazepine dimer (IGN) payloads are used in several clinical-stage antibody–drug conjugates. IGN drugs alkylate DNA through the single imine moiety present in the dimer in contrast to the pyrrolobenzodiazepine dimer drugs, such as talirine and tesirine, which contain two imine moieties per dimer and cross-link DNA.

This study explored the mechanism of binding of IGN. A number of studies have confirmed that alkylation of DNA by nitrogen mustards passes through the formation of aziridinium ion.The first step of the alkylation reaction involves donation of a lone pair of electron from the N-center of the nitrogen mustard to the chloroethyl side chain with the release of a chloride ion (Cl −), forming an aziridinium (Az +) ion (step 1, Scheme 1).

Subhas Bose D, Thompson AS, Ching J, Hartley JA, Berardini MD, Jenkins TC, Neidle S, Hurley LH, Thurston DE. Rational design of a highly efficient non-reversible DNA interstrand cross-linking agent based on the pyrrolobenzodiazepine ring system.

J Am. PS-DNA failed to form a triple helix of the type d(T) n d(A) n d(T) n, and resulted in the dissociation of the PS-DNA duplex and reformation of a triple helix based upon an anti-PS-DNA duplex core d(T) 10 d(A) Cellular and pharmacological studies In vitro studies.

Interaction of psoralen-derivatized oligodeoxyribonucleoside methylphosphonates with single-stranded DNA. Ruthenium(II) polypyridine complexes are one of the most extensively studied and developed systems in the family of luminescent transition-metal complexes.

Notably, there has been a large amount of interest in the biological applications of these luminescent ruthenium(II) complexes because of their rich photophysical and photochemical properties. In this Viewpoint, we explore past and recent. Book Reviews Methods in Biotechnology 4: Natural Products Isolation Edited by Richard J.

Cannell. Humana Press, Totowa, NJ. x + pp. 15 x cm. ISBN $. "This book covers clinically used anticancer agents that are either natural products or are clearly derived from natural product leads.

The second edition includes drugs that are currently in development. In addition, the text emphasizes the applications of synthetic and medicinal chemistry to the preparation of analogs with enhanced activities.The synthesis and biological evaluation of phosphate prodrugs of analogues of 1 (CC) and their conjugates with antibodies are described.

The phosphate group on the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indolone (CBI) portion of the compounds confers enhanced solubility and stability in aqueous solutions.

In the presence of phosphatases, these compounds convert into active DNA. Pepper, C.J. et al., “The novel sequence-specific DNA cross-linking agent SJG (NSC ) has potent and selective in vitro cytotoxicity in human B-cell chronic lymphocytic leukemia cells with evidence of a pindependent mechanism of cell kill,” Cancer Res.

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