Ionophoric activity of acyl and alkyl derivatives of 2,3-benzo-15-crown-5

Shkinëv, A. V.; Gagel’gans, A. I.; Ташмухамедова, А. К.; Tashmukhamedov, B.A.

doi:10.1007/bf00570818

Cited by 3 publications

(2 citation statements)

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“…Table I11 for 9 successive days from day one. 29,No. 7 1255 N ,N:N',N'-Bis[ 2-met hyl-1,2-propanediyl]phosphorodiamidothioate (5d). The anticancer activity was evaluated by comparing the mean survival time of treated with that of the control animals, i.e., by the T I C method where Materials.…”

Section: Methodsmentioning

confidence: 99%

“…29 While no visible signs of a reaction were observed with linear polyether derivatives 5a-d, the reactions of the crown compounds 7a-d resulted instantly in a turbidity, which slowly changed to a precipitate of white crystalline products 8a-d in 18-69% yields. 29 While no visible signs of a reaction were observed with linear polyether derivatives 5a-d, the reactions of the crown compounds 7a-d resulted instantly in a turbidity, which slowly changed to a precipitate of white crystalline products 8a-d in 18-69% yields.…”

Section: Chemistrymentioning

confidence: 99%

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In the search for new anticancer drugs. 17. Linear and cyclic polyether analogs of N,N:N',N':N",N"-tri-1,2-ethanediylphosphoric triamide and N,N:N',N':N",N"-tri-1,2-ethanediylphosphorothioic triamide

Sosnovsky¹,

Lukszo²,

Rao³

1986

J. Med. Chem.

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Linear and cyclic polyether derivatives of N,N:N',N':N'',N''-tri-1, 2-ethanediylphosphoric triamide (TEPA) and N,N:N',N':N'',N''-tri-1,2-ethanediylphosphorothioic triamide (thio-TEPA) are synthesized and evaluated for their antineoplastic activity against the murine lymphocytic leukemia P388. All compounds, except for 7d, were active ranging from 42% to 287% increase in life span (% ILS). All CD2F1 male mice treated with the most active compound (7a) at 90 mg/kg per day for 9 days were alive after 30 days, whereas all mice treated with the clinical drug thio-TEPA were dead. The % ILS for compound 7a on day 60 was 525. A correlation is presented between the structural features of compounds and their lipophilicities and antineoplastic activities.

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Section: Methodsmentioning

confidence: 99%

Section: Chemistrymentioning

confidence: 99%

In the search for new anticancer drugs. 17. Linear and cyclic polyether analogs of N,N:N',N':N",N"-tri-1,2-ethanediylphosphoric triamide and N,N:N',N':N",N"-tri-1,2-ethanediylphosphorothioic triamide

Sosnovsky¹,

Lukszo²,

Rao³

1986

J. Med. Chem.

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Transport of alkali cations through thin lipid membranes by (222)C10-Cryptand, an ionizable mobile carrier

Castaing¹,

Morel²,

Lehn

1986

J. Membrain Biol.

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The kinetics of K+ and Na+ transport across the membrane of large unilamellar vesicles (L.U.V.) were compared at two pH's, with two carriers: (222)C10-cryptand (diaza-1,10-decyl-5-hexaoxa-4,7,13,16,21,24-bicyclo[8.8.8.]+ ++hexacosane) and valinomcyin, i.e. an ionizable macrobicyclic amino polyether and a neutral macrocyclic antibiotic. The rate of cation transport by (222)C10 saturated as cation and carrier concentrations rose. The apparent affinity of (222)C10 for K+ was higher and less pH dependent than that for Na+ but resembled the affinity of valinomycin for K+. The efficiency of (222)C10 transport of K+ decreased as the pH fell and the carrier concentration rose, and was about ten times lower than that of valinomycin. Noncompetitive K+/Na+ transport selectivity of (222)C10 decreased as pH, and cation and carrier concentrations rose, and was lower than that of valinomycin. Transport of alkali cations by (222)C10 and valinomycin was noncooperative. Reaction orders in cation n(S) and carrier m(M) varied with the type of cation and carrier and were almost independent of pH; n(S) and m(M) were not respectively dependent on carrier or cation concentrations. The apparent estimated constants for cation translocation by (222)C10 were higher in the presence of Na+ than of K+ due to higher carrier saturation by K+, and decreased as pH and carrier concentration increased. Equilibrium potential was independent of the nature of carrier and transported cation. Results are discussed in terms of the structural, physiocochemical and electrical characteristics of carriers and complexes.

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