Cyclams

10/01/2020 - "We synthesized 6 iodinated and brominated cyclam derivatives with high affinity (low nM range) for CXCR4, since structure-based estimates of lipophilicity suggested rapid transfer across the BBB and tumor cell membranes. "
01/21/2002 - "Two new lipophilic tetraazamacrocycles were prepared and, in contrast to non-lipophilic analogs, found to be potent inhibitors of tumor cell growth in vitro with IC50 values below 10 micromolar."
08/01/2014 - "The biodistribution and PET/CT imaging studies with the radiolabeled bridged cyclams demonstrated longer tumor retention and comparable uptake to [(64)Cu]AMD3465, though [(64)Cu]AMD3465 demonstrated superior overall pharmacokinetics. "
06/01/2002 - "These data suggest that some azomycin-cyclams exhibit good hypoxia-marking potential to tumor cells in vitro and to animal tumors of known RHF. "
05/01/2001 - "In an attempt to generate new platinum compounds that may be effective in the treatment of cancer, as well as having a lower toxicity than traditional platins and being orally viable, we are studing the synthesis and reactivity of platinum complexes of tetraazamacrocycles bearing carboxylato pendant arms. "

05/01/2000 - "Inhibition of HIV infection by bicyclams, highly potent and specific CXCR4 antagonists."
03/01/1996 - "The results presented here provide further support for the bicyclams as attractive candidate drugs for the chemotherapy of HIV infections."
03/01/1996 - "As described in this paper, PCR experiments revealed that no viral DNA was formed following viral infection, thus confining the target(s) of action of the bicyclams to an early stage of HIV infection. "
05/01/2000 - "The bicyclams represent a new entity of low-molecular weight molecules that inhibit human immunodeficiency virus (HIV) infection through a specific blockade of CXCR4 (fusin), the receptor for the CXC chemokine SDF-1 (soluble-derived factor), which is also used as coreceptor by T-lymphotropic HIV strains to enter their target cells. "
08/01/2005 - "This is illustrated by a number of representative examples: S-adenosylhomocysteine (SAH) hydrolase inhibitors which display broad-spectrum antiviral activity, bromovinyldeoxyuridine (BVDU) and derivatives thereof, that are highly selective inhibitors of varicella-zoster virus (VZV), (dideoxy)nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs) which are now widely used in the treatment of HIV infections (AIDS), the bicyclams (i.e. "

03/01/1996 - "As described in this paper, PCR experiments revealed that no viral DNA was formed following viral infection, thus confining the target(s) of action of the bicyclams to an early stage of HIV infection. "
10/01/2001 - "In the search of effective and selective chemotherapeutic agents for the treatment of viral infections, my "Odyssey" brought me to explore a variety of approaches, encompassing interferon and interferon inducers, suramin and other polyanionic substances, S-adenosylhomocysteine hydrolase inhibitors, inosine 5'-monophosphate dehydrogenase inhibitors, 5-substituted 2'-deoxyuridines such as (E)-5-(2-bromovinyl)-2'-deoxyuridine, acyclovir (esters) and other acyclic guanosine analogues, 2',3'-dideoxynucleoside analogues, non-nucleoside reverse transcriptase inhibitors (NNRTIs), bicyclams, and acyclic nucleoside phosphonates. "

07/01/2001 - "Importantly, compared with the wild-type receptor, CXCR4[D262N] was much less effective, whereas CXCR4[D171N,D262N] completely failed as a coreceptor for infection by HIV-1 NL4.3. Thus, the negatively charged aspartate residues at positions 171 and 262, located in transmembrane domains 4 and 6 of the 7-transmembrane receptor, respectively, may represent crucial sites for electrostatic interaction of the positive charges of the bicyclams, as well as for the highly basic V3 loop of the gp120 envelope protein of certain HIV-1 strains."
11/01/2000 - "The octapeptide D-Ala-Ser-Thr-Thr-Thr-Asn-Tyr-Thr-NH(2) ([D-Ala(1)]TNH(2)), an analog of peptide T (H-Ala-Ser-Thr-Thr-Thr-Asn-Tyr-Thr-OH) associated with CD(4)/T(4) receptors involved in human immunodeficiency virus infection, was combined with the chelating polyazamacrocycle 1,4,8,11-tetraazacyclotetradecane (cyclam) to afford the bifunctional ligand cyc-[D-Ala(1)]TNH(2). "

06/01/2002 - "FC-327 and FC-334, di-azomycin-substituted cyclams, exhibited hypoxia-specific factors > or = 7.0. "
06/01/2002 - "These data suggest that some azomycin-cyclams exhibit good hypoxia-marking potential to tumor cells in vitro and to animal tumors of known RHF. "
11/04/2004 - "The novel Cu(II) complexes of N-mustard derivatives of 1,4,7-triazacyclononane (tacn), 1,4,7,10-tetraazacyclododecane (cyclen), and 1,4,8,11-tetraazacyclotetradecane (cyclam) were assessed in vitro as hypoxia-selective cytotoxins. "