Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Spiro Compounds”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 199 records · Page 11Linked to original sources
PubMed1986

[Metastatic cancer of the prostate: phase II study of spirogermanium (NSC 192965)].

A phase II study of spirogermanium was conducted in a series of 15 patients with metastatic prostatic carcinoma. All the patients have previously received multiple hormonal therapies. The drug was administered at the dose of 200 mg/m2 by a continuous infusion for five days, and 120 mg/m2, three times a week subsequently. The side effects were mainly neurological toxicity and phlebitis at the injection points which were dose and schedule dependent. Only one partial response for two months was noted in this series. Thus, spirogermanium seems to have a limited value in patients with prostatic cancer.

Aged↗
PubMed1983

Spirogermanium: a new drug with antimalarial activity against chloroquine-resistant Plasmodium falciparum.

Spirogermanium, a new investigational drug of novel structure currently under clinical studies in various neoplastic diseases, has revealed significant in vitro activity against chloroquine-resistant (FCB, FTA, FVO) and sensitive (FSL, FUI, FH) strains of Plasmodium falciparum. Inhibition of the growth and maturation of parasites after 36-h exposures to Spirogermanium started at concentrations ranging from 2.48 to 9.9 nM/ml. These concentrations appear to be within the range of Spirogermanium plasma levels reported in clinical studies with this drug. Since its clinical toxicities are unusually low in comparison with other anticancer drugs, our results on its in vitro activity against Plasmodium falciparum indicate Spirogermanium is an antimalarial drug of entirely novel structure, active in resistant strains.

Antimalarials↗
PubMed1982

Cytotoxic effects and biological activity of 2-aza-8-germanspiro[4,5]-decane-2-propanamine-8,8-diethyl-N,N-dimethyl dichloride (NSC 192965; spirogermanium) in vitro.

Lethal and other biological effects of 2-aza-8-germanspiro[4,5]decane-2-propanamine-8,8-diethyl-N,N-dimethyl dichloride (NSC 192965; spirogermanium), representing a new chemical class of compound exhibiting antitumor activity, have been studied in vitro. Survival curves for NIL 8 hamster cells were exponential with greater kill occurring with increasing drug concentrations and longer exposure times. Cytotoxicity was temperature dependent. "Quiescent" cultures were significantly less sensitive to spirogermanium than were logarithmically growing cells. These lethal effects showed no phase specificity. There was no evidence of progression delay through the cycle following spirogermanium treatment. When spirogermanium was tested against a range of human cell lines, the consistency of the values for the drug concentration required to reduce survival by 50% on the exponential part of the survival curve, derived from colony-forming assays, was most marked. The survival curves, characterized by an initial shoulder, were steep and exponential with measurements possible over only a narrow concentration range since complete cell lysis occurred at levels causing a greater than 2-log kill. Cell membrane damage by spirogermanium, as judged by dye exclusion, was progressive with time and increasing drug concentrations. Protein synthesis proved most susceptible to the drug. Spirogermanium concentrations cytotoxic to tumor cells were also toxic to cultured rat neurons, confirming the clinical neurological toxicity encountered. The precise mode of action of spirogermanium remains to be established, and these data further illustrate its apparent lack of specificity.

Animals↗
PubMed2005

Highly fluorescent solid-state asymmetric spirosilabifluorene derivatives.

A series of four asymmetrically aryl-substituted 9,9'-spiro-9-silabifluorene (SSF) derivatives, 2,2'-di-tert-butyl-7,7'-diphenyl-9,9'-spiro-9-silabifluorene (PhSSF), 2,2'-di-tert-butyl-7,7'-dipyridin-2-yl-9,9'-spiro-9-silabifluorene (PySSF), 2,2'-di-tert-butyl-7,7'-dibiphenyl-4-yl-9,9'-spiro-9-silabifluorene (BPhSSF), and 2,2'-di-tert-butyl-7,7'-bis(2',2' '-bipyridin-6-yl)-9,9'-spiro-9-silabifluorene (BPySSF) are prepared through the cyclization of the corresponding 2,2'-dilithiobiphenyls with silicon tetrachloride. These novel spiro-linked silacyclopentadienes (siloles) form transparent and stable amorphous films with relatively high glass transition temperatures (T(g) = 203-228 degrees C). The absorbance spectrum of each compound shows a significant bathochromic shift relative to that of the corresponding carbon analogue as a result of the effective sigma-pi conjugation between the sigma orbital of the exocyclic Si-C bond and the pi orbital of the oligoarylene fragment. Solid-state films exhibit intense violet-blue emission (lambda(PL) = 398-415 nm) with high absolute photoluminescence quantum yields (phi(PL) = 30-55%).

Biphenyl Compounds↗
PubMed1994

Structural investigation of the new potent DNA alkylator spiro(2H-1,3,2-benzodiazaphosphole-2,2',lambda 5 [1,3,5,2,4,6] triazatriphosphorine),4',4',6',6'-tetrakis(1-aziridinyl)-1,3,4',4',6', 6',-hexahydro.

The molecular structure of spiro(2H-1,3,2-benzodiazaphosphole-2,2',lambda 5 [1,3,5,2,4,6] triazatriphosphorine), 4',4',6',6'-tetrakis(1-aziridinyl)-1,3,4',4',6',6'-hexahydro (CAS 133586-94-4), a recently synthesized potent cytostatic, was determined using X-ray diffraction method. The substance crystallizes in P2(1)2(1)2(1) orthorhombic space group. The unit cell contains 8 formal molecules coupled into 4 pseudo-centrosymmetric dimers by double intermolecular hydrogen bonds. The compound revealed, besides previously determined long-term chemical stability and good water solubility, also radiation stability. In spite of having less aziridinyl groups than 1,3,5,2,4,6-triazatriphosphorine,2,2,4,4,6,6-hexakis (1-aziridinyl)-2,2,4,4,6,6-hexahydro (N3P3Az3, Az = aziridinyl, CAS 52-46-0; Myko 63) the compound is twice more cytostatically active. Hypotheses attributing high cytostatic activity to the existence of conjugated pi-electron systems in the molecule and dimeric structures are discussed.

Alkylating Agents↗
PubMed2006

Efficient approach to the Azaspirane core of FR 901483.

[reaction: see text] An efficient approach to the azaspirane core of FR 901483 is described employing lithiated methoxyallene as a crucial C3 building block and a suitably protected enantiopure ketimine as the second component. The resulting dihydropyrrole derivative was smoothly converted into a spiro keto aldehyde which under acidic conditions provided a novel azanorbornane derivative 15. Under basic reaction conditions, the desired 5-azatricyclo[6.3.1.0(1,5)]dodecane skeleton 16 was generated. The ratio of diastereomers strongly depends on the reaction conditions employed with l-proline in DMSO providing the highest selectivity in favor of one azaspirane product.

Catalysis↗